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SML1187   Vacquinol-1 dihydrochloride ≥98% (HPLC) Vacquinol-1 (NSC13316) is a brain penetrant inducer of catastrophic vacuolization in glioblastoma cells (GCs). Vacquinol-1 displays high cytotoxicity to GCs; it induces cell death by membrane ruffling, cell rounding, massive macropinocytic vacuole accumulation, ATP depletion, and cytoplasmic membrane rupture of GCs. Vacquinol-1 originally was developed as an antimalarial compound.
Vacquinol-1 dihydrochloride is potentially used as a therapeutic for Glioblastoma multiforme (GBM). This drug is highly stable in vivo, with a half-life in plasma of 52 hour. Vacquinol-1 has high oral bioavailability and good brain penetration.
SML0011 VAHA ≥98% (HPLC) Hydroxamic acid derivatives of valproic acid exhibit anticonvulsant activity with no teratogenic activity in mouse neural tube defect model. It is effective in the treatment of bipolar disorders.
VAHA (Valproyl hydroxamic acid) is an HDAC inhibitor with less activity than valproic acid against Class I enzymes but much greater Class II activity
PZ0179 Valdecoxib ≥98% (HPLC) Valdecoxib is a non-steroidal anti-inflammatory drug (NSAID), a cyclooxygenase-2 (COX-2) selective inhibitor.
Valdecoxib is reported to elicit anti-inflammatory, analgesic and antipyretic functionality. It acts as a substrate for the liver enzyme cytochrome P450 2C9(CYP2C9) and cytochrome P450 3A4 (CYP3A4).
human ... PTGS2(5743)
V2889 Valeryl Salicylate ≥98% (HPLC) Selective, irreversible COX-1 inhibitor. The selectivity for COX-1 vs COX-2 shows the IC50 values for ovine COX-1 vs COX-2 of 0.8 μM vs. 15 mM respectively.
SML0191 Valganciclovir hydrochloride hydrate ≥98% (HPLC) Valganciclovir hydrochloride hydrate is an antiviral used to treat cytomegalovirus infection. It is the prodrug of ganciclovir, a synthetic analog of 2′-deoxy-guanosine which is phosphorylated to a dGTP analog that competitively inhibits the incorporation of dGTP by viral DNA polymerase.
Valganciclovir is a valine ester of Ganciclovir, used to treat cytomegalovirus retinitis in HIV-infected patients. It is rapidly metabolized to ganciclovir by hydrolysis before entering the systemic circulation resulting in improved absorption of the drug.
V0627 Valinomycin ≥98% (TLC), ≥90% (HPLC) K+-selective ionophoric cyclodepsipeptide; potassium ionophore which uncouples oxidative phosphorylation, induces apoptosis in murine thymocytes, inhibits NGF-induced neuronal differentiation and antagonizes ET-induced vasoconstriction.
V4765 Valnoctamide ≥98% (NMR) Valnoctamide exhibits anti-cytomegalovirus (anti-CMV) properties. It has therapeutic effects against status epilepticus (SE) and neuropathic pain. Valnoctamide also shows therapeutic effects against bipolar disorders.
Valproic acid (VPA) and derivatives such as valpromide and valnoctamide are anti-convulsant, mood stabilizing drugs, believed to function as indirect GABA agonists by inhibiting the transamination of GABA.
P4543 Valproic acid sodium salt 98% Anti-convulsant that also has efficacy as a mood stabilizer in bipolar disorder.
Valproic acid is an anticonvulsant and mood-stabilizing drug. It is used to treat epilepsy and bipolar disorder. Valproic acid helps to repress the Warburg effect and the development of tumor in neuroblastoma.
human ... ALDH5A1(7915)
V3640 Valpromide ≥97% (NMR) Valpromide (VPD) is a derivative of valproic acid (VPA) and is used as an antiepileptic drug. It is hydrolyzed quickly to VPA in vivo, but has intrinsic anticonvulsant activity.
Valpromide possesses antipsychotic property. It lacks the toxic and teratogenic effects of valproic acid. It also lacks the histone deacetylase (HDAC) inhibitory activity of valproic acid.
SML0142 Valsartan ≥98% (HPLC) Valsartan is an Angiotensin II type 1 (AT1) receptor antagonist and anti-hypertensive. Valsartan renders protection against heart attack and stroke resulting from abrupt increase in blood pressure. Valsartan reduces myocardial-infarction-related complications in heart attack survivors.
human ... AGTR1(185)
SML0572 Valspodar ≥98% (HPLC) Valspodar is a nonimmunosuppressive cyclosporin analog and potent P-glycoprotein (MDR1) inhibitor. Valspodar reverses multidrug resistance (MDR) by inhibiting cellular drug efflux mediated by P-glycoprotein.
SML2983 Vandetanib ≥98% (HPLC) New Vandetanib is an orally active and potent inhibitor of vascular endothelial growth factor receptor receptor 2 (VEGFR2) kinase activity that is used to treat medullary thyroid cancer. Vandetanib also inhibits epidermal growth factor receptor (EGFR), and RET tyrosine kinases.
V9130 N-Vanillylnonanamide ≥97%, powder   rat ... Trpv1(83810), Trpv4(66026)
SML2103 Vardenafil hydrochloride trihydrate ≥98% (HPLC) Vardenafil is a potent, selective inhibitor of cGMP specific phosphodiesterase type 5 (PDE5). It is used clinically to treat erectile dysfunction.
PZ0004 Varenicline tartrate ≥98% (HPLC) Varenicline tartrate is a partial α4β2 nicotinic receptor agonist and α7 full agonist. Varenicline competitively binds to α4β2 receptors and partially stimulates without creating a full nicotine effect, while simultaneoudly blocking the ability of nicotine to bind to the receptors. Varenicline thus blocks the ability of nicotine to activate α4β2 receptors and stimulate the central nervous mesolimbic dopamine system, believed to be the neuronal mechanism underlying reinforcement and reward experienced upon smoking.
SML1100   Varespladib ≥98% (HPLC) Varespladib is a potent and selective inhibitor of secretory phospholipase A2 (sPLA2). The compound Varespladib inhibits both human and mouse sPLA2 group IIA, V, and X enzymes at low nM concentrations.
SML0273 VAS2870 ≥97% (HPLC) In addition to NOX4 inhibition, VAS2870 is also known to supress the reactive oxygen species (ROS) production in several cell types. It effectively impairs cell growth and increases apoptosis induced by transforming growth factor β (TGF-β) in liver cancer cells. Thus, inhibition of NOX enzymes by VAS2870 may be considered as a potential therapeutic strategy for liver cancer.
VAS2870 is a cell-permeable and specific NADPH oxidase (NOX) inhibitor that effectively suppresses growth factor-mediated ROS liberation in VSMC.
SML2498 Vatalanib dihydrochloride ≥98% (HPLC) Vatalanib (PTK787, ZK 222584, CGP 79787D, CGP 79787 succinate) is an orally active anilinophthalazine derivative that exerts its anti-angiogenic efficacy by targeting receptor tyrosine kinase (RTK) VEGFR (VEGFR1/2 IC50 = 54/39 nM; IC50 ∼30 nM against 100 ng/mL VEGF-C-induced VEGFR3 autophosphorylation in MEVCs) and, to a less extent, PDGFRβ, c-kit, c-fms (IC50 = 364, 600, 567 nM, respectively) in an ATP-competitive manner with much reduced or no potency toward >90 other kinases. Typical dosing ranges: 0.1-10 μM in cultures, 5 nM-200 μM (zebrafish) and 30-100 mg/kg (mice & rats via po. or ip) in vivo.
V3264 VDM 11 ≥98% (HPLC), oil Potent, selective anandamide membrane transporter (AMT) inhibitor.
SML0063 Q-VD-OPh hydrate ≥95% (HPLC) Q-VD-OPh is a potent pan-caspase inhibitor that protects cells from capsase-dependent apoptosis. Q-VD-OPh has superior aqueous stability, cell permeability, and efficacy than FMK-based caspase inhibitors and displays no cytotoxic effects alone.
SML1415 VE-821 ≥98% (HPLC) VE-821 is a potent ATP-competitive inhibitor of the DNA damage response (DDR) kinase Ataxia telangiectasia-mutated (ATM) and ATM- and Rad3-related (ATR) with a Ki of 13 nM. VE-821 has minimal cross-reactivity against the related PIKKs ATM, DNA-dependent protein kinase (DNA-PK), mTOR and PI3-kinase-γ (Ki of 16 μM, 2.2 μM, >1 μM and 3.9 μM, respectively) and against a large panel of unrelated protein kinases. VE-821 used alone caused death in a large fraction of cancer cell populations and also showed strong synergy with genotoxic agents. VE-821 increased sensitivity of cells to radiation and also sensitized cancer cells to a variety of chemotherapeutic agents.
V7264 Venlafaxine hydrochloride ≥98% (HPLC), powder Venlafaxine is an antidepressant. The mechanism of the antidepresant action of venlafaxine in humans is associated with its potentiation of neurotransmitter activity in the CNS. Venlafaxine is a potent inhibitor of neuronal serotonin and norepinephrine reuptake and weak inhibitor of dopamine reuptake. Venlafaxine has no significant activity for muscarinic, histaminergic, or α-1 adrenergic receptors in vitro. Venlafaxine does not possess MAO inhibitor activity.
human ... SLC6A2(6530), SLC6A4(6532)
SML0271 VER-155008 ≥98% (HPLC) VER-155002 is a small molecule, ATP-derivative inhibitor of HSP70 (IC50 = 500 nM). The compound inhibits proliferation of several colon and breast cancer cell lines, induces caspase dependent apoptosis in BT474 cells and down regulates expression of Her2 and Raf-1 in HCT116 cells.
VER‐155008 positively promotes memory recovery and axonal regrowth. It is also involved in inhibiting cell cycle progression and proliferation in non-small-cell lung cancer (NSCLC).
V4629 (±)-Verapamil hydrochloride ≥99% (titration), powder α1-adrenoceptor antagonist; L-type calcium channel blocker. Blocks L-type Ca2+ channels in smooth and cardiac muscle, induces apoptosis of human primary and metastatic colon adenocarcinoma cells in vitro. Drug resistance reversal agent acting on Pgp, e.g. decrease renal tubule elimination of digoxin. Increases basal ATPase activity of Pgp. Substrate of Cyp3A4 and CYP2C6.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146), CACNA1C(775), CACNA1D(776), CACNA1F(778), CACNA1S(779)
V106 R(+)-Verapamil monohydrochloride hydrate ≥98% (HPLC), powder Inhibitor of P-glycoprotein; less active enantiomer of (±)-verapamil.
Verapamil is a calcium channel blocker. Verapamil hydrochloride is a phenyl-alkyl amine derivative and is potentially used for treating hypertension, angina pectoris and arrhythmias. It is water soluble in nature.
V105 S(−)-Verapamil hydrochloride hydrate ≥98% (HPLC), powder Active enantiomer of (±)-verapamil. Ca2+ channel (L-type) modulator; adrenoceptor antagonist; cardiac depressant.
V5754 Veratridine ≥90% (HPLC), powder Opens voltage-dependent Na+ channels and prevents their inactivation. This, in turn, opens voltage-activated calcium channels, thus increasing intracellular calcium content and inducing neurotransmitter release. Alkaloid neurotoxin which depolarizes excitable tissue; used to increase membrane sodium permeability. Veratridine is cytotoxic to chromaffin cells in vitro.
Veratridine has been used as an insecticide, acting as a paralytic agent with higher toxicity to insects than to mammals.
SML2938   Vernakalant hydrochloride ≥98% (HPLC) New Vernakalant is a multiple ion channel blocker that exerts in vivo anti-fibrillatory (anti-arrhythmic) efficacy (ED50 = 1.5 μmol/kg/min iv. against ischemia-induced arrhythmias in rats) via atrial-selective Kv1.5 blockage (hKv1.5/rKv4.2/rKv4.3 IC50 = 13/38/30 μM at 1Hz & -80 to 60 mV in 200 (Kv1.5) or 400 (Kv4) msec) as well as potential- and rate-dependent Nav1.5 blockade (inward Na current INa IC50 = 9 μM/20 Hz & -80 mV, 31 μM/1Hz & -60 mV, 107 μM/1Hz & -120 mV using HEK hNav1.5 cells).
V4877 Verrucarin A from Myrothecium sp. ≥85.0% (HPLC) Verrucarin A binds to the P and A sites in ribosomes and blocks peptide-bond and translation initiation. It inhibits the clear cell renal cell carcinoma (CCRCC) proliferation. Verrucarin A blocks the peptidyl transferase activity and favors apoptosis induction in cancer cells
Verrucarin A is phytotoxic to plantlet cultures and cytotoxic to cultured mammalian cell lines.
V1628 Verrucarol Trichothecene mycotoxin that is a component of toxic mold. Esters of verrucarol have anti-tumor activity.
SML0534 Verteporfin ≥94% (HPLC) Verteporfin has an ability to disrupt the interaction between YAP (Yes-associated protein)/TAZ (transcriptional coactivator with PDZ-binding motif) and TEA domain (TEAD) complex. It also reduces the viability of the ovarian cancer cells and almost eliminates cell migration. Therefore, verteporfin might be considered as a potent therapeutic for ovarian cancer.
Verteporfin is a photosensitizer for photodynamic therapy to eliminate the abnormal blood vessels in the eye associated with conditions such as macular degeneration. Verteporfin accumulates in abnormal blood vessels and, when stimulated by nonthermal red light with a wavelength of 693 nm in the presence of oxygen, produces highly reactive short-lived singlet oxygen and other reactive oxygen radicals, resulting in local damage to the endothelium and blockage of the vessels. Verteporfin localizes predominantly in mitochondria.
SML1896 VH298 ≥98% (HPLC) VH298 is a cell-permeable small molecule that disrupts the interaction of VHL with Hypoxia-inducible factor HIF-α, stabilizing HIF-α and inducing a hypoxic response. Hypoxia-inducible factors (HIFs) are oxygen-sensitive transcription factors that regulate hypoxic signalling. They are regulated by oxygen-dependent prolyl hydroxylase domain (PHD) enzymes and polyubiquitination by the von Hippel–Lindau (VHL) Cullin RING E3 ubiquitin ligase complex. Unlike many PHD inhibitors, which have off-target effects, VH298 acts downstream of the PHD enzymes, inhibiting the VHL:HIF-α interaction. VH298 had a Kd of 90 nM. VH298 was shown to induce HIF transcriptional activity, to increase accumulation of HIF-α in HeLa cells and to stimulate erythropoietin production in RCC4 cells.
SML2768 Vicriviroc Maleate ≥98% (HPLC) Vicriviroc is an orally available, potent and selective allosteric antagonist of C-C chemokine CCR5 receptors. Vicriviroc inhibits the interaction of HIV-1 with CCR5 receptor thereby preventing HIV-1 virus entry into cells.
V8261 (±)-Vigabatrin Irreversible GABA transaminase inhibitor. Increases intracellular concentration of GABA in nerve endings; possesses antiepileptic activity.
human ... ABAT(18), GABBR1(2550), GABBR2(9568), GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA4(2557), GABRA5(2558), GABRA6(2559), GABRB1(2560), GABRB2(2561), GABRB3(2562)
V113 S(+)-γ-Vigabatrin solid GABA transaminase inhibitor; anti-convulsant.
γ-Vigabatrin has the potential to treat infantile spasms and seizures. It exhibits therapeutic effects against cocaine and other addictions.
SML1098 Vilazodone hydrochloride ≥98% (HPLC) Vilazodone is a serotonin 5-HT1A partial agonist and serotonin-selective reuptake inhibitor (SPARI) that is used clinically as an antidepressant for major depressive disorder.
human ... HTR1A(3350), SLC6A4(6532)
SML2302 Vildagliptin ≥98% (HPLC) Vildagliptin ia a selective inhibitor of dipeptidyl peptidase 4 (DPP4). This enzyme breaks down the incretins GLP-1 and GIP, gastrointestinal hormones that are released in response to a meal. By preventing GLP-1 and GIP inactivation, GLP-1 and GIP are able to potentiate the secretion of insulin and suppress the release of glucagon by the pancreas.
V1377 Vinblastine sulfate salt ≥97% (HPLC) Plant alkaloid that inhibits microtubule assembly by binding tubulin and inducing self-association in spiral aggregates in a reaction that appears to be regulated by the C-terminus of β-tubulin and is enhanced by GDP and GTP. Depolymerizes microtubules. Arrests the cell cycle in G2/M-phase by blocking mitotic spindle formation. Triggers Raf-1 activation, phosphorylation of bcl-2-family proteins, induction of p53 expression, and apoptosis in several tumor cell lines. Substrate of Pgp and CYP3A4.
human ... TBCC(6903), TUBA1A(7846), TUBA1B(10376), TUBA1C(84790), TUBA3C(7278), TUBA3E(112714), TUBA4A(7277), TUBB(203068), TUBB1(81027), TUBB2A(7280), TUBB2B(347733), TUBB3(10381), TUBB4A(10382), TUBB4B(10383), TUBB6(84617), TUBB8(347688)
V4890 Vindesine sulfate salt hydrate ≥95% (HPLC) Microtubule inhibitor. Vindesine binds to and stabilizes tubulin, thereby preventing tubulin polymerization, preventing mitosis, and arresting cells in metaphase.
V2264 Vinorelbine ditartrate salt hydrate ≥98% (HPLC), powder Vinorelbine is a potent anti-mitotic, anti-tumor agent. Vinorelbine inhibits microtubule assembly. Low neurotoxicity is related to its higher affinity for mitotic microtubules than for axonal microtubules.
V6383 Vinpocetine ≥98%, solid Ca2+-calmodulin-dependent phosphodiesterase I (PDE1) inhibitor.
human ... PDE1A(5136), PDE1B(5153), PDE1C(5137)
V9389   Violacein from Janthinobacterium lividum >98% (violacein (minimum 85% violacein) and deoxyviolacein, HPLC) Violacein, a violet pigment, is an indole derivative produced by various bacterial strains such as Chromobacterium violaceum, Janthinobacterium lividum, Chromobacterium lividum, and Pseudoalteromonas luteoviolacea. Violacein is a member of a novel class of cytotoxic drugs, which mediate apoptosis. Violacein exhibits antitumoral, antibacterial, antiulcerogenic, antileishmanial, and antiviral activities. Violacein and its β-cyclodextrin complexes trigger apoptosis and differentiation in HL60 leukemic cells. Violacein cytotoxicity is preceded by activation of caspase 8, transcription of NF-κB target genes, and p38-MAPK activation resembling TNF-α signal transduction.
SML0367 VK3-OCH3 ≥98% (HPLC) VK3-OCH3 is an analog of Vitamin K3 (Menadione) with potent antitumor activity. It has been shown to induce G2/M arrest and apoptosis in neuroblastoma cells with much less cytotoxicity towards normal cells. VK3-OCH3 is believed to act through up-regulation of heme oxygenase (HO)-1.
V8639 VO-OHpic trihydrate ≥98% (HPLC), solid VO-OHpic trihydrate is a PTEN (phosphatase and tensin homologue deleted on chromosome 10) inhibitor.
PZ0005 Voriconazole ≥98% (HPLC) Voriconazole is an antifungal used to treat serious fungal infections. Voriconazole inhibits ergosterol synthesis by inhibiting CYP450-dependent 14-α sterol demethylase resulting in a depletion of ergosterol in fungal cell membranes.
Voriconazole is used to treat invasive aspergillosis (IA). It is vigorous against Candida species, including the strains of Candida albicans, which shows resistance to fluconazole.
SML1823 Vosaroxin hydrochloride ≥98% (HPLC) Vosaroxin is an anti-cancer quinolone derivative that acts as a DNA intercalator and a topoisomerase II inhibitor, causing p53 independent tumor cell apoptosis. Vosaroxin stabilizes cleavage complexes formed by topoisomerase IIα and IIβ, which results in an accumulation of DNA double-strand breaks. Vosaroxin showed antineoplastic activity in multiple solid tumor and hematologic cancer cell lines and has been in clinical trials for AML.
SML1886 VPC-13566 ≥98% (HPLC) VPC-13566 is Binding Function 3 (BF3)-specific inhibitor of the androgen receptor. VPC-13566 potently inhibits AR transcriptional activity by displacement of the BAG1L peptide from the BF3 pocket. VPC-13566 inhibits the growth of various prostate cancer cell lines including an enzalutamide-resistant cell line and inhibits the growth of AR-dependent prostate cancer xenograft in mice.
SML1544 VPC-14228 ≥98% (HPLC) VPC-14228 is a potent and specific inhibitor of human androgen receptor (AR) that binds to AR DNA-binding domain (AR DBD). Apparently VPC-14228 blocks the transcriptional activity of constitutively active AR splice variants.
SML1599   VR23 ≥98% (HPLC) Proteasomes are responsible for the cleavage of peptides in an ATP/ubiquitin-dependent manner.
VR23 is a potent inhibitor of proteasome that primary targets β2 of the 20S proteasome catalytic subunit. VR23 selectively induces apoptosis to cancer cells via cyclin E–mediated centrosome amplification. VR23 exhibit little effect on noncancerous cells.
V2390   VRT-532 ≥98% (HPLC) VRT-532 is a mutated G551D CFTR corrector. VRT-532 mediates G551D-CFTR by enhancement of ATP affinity of the mutant. VRT-532 also potentiates F508del mutated CFTR and works specifically on mutant CFTR rather than other membrane proteins.
SML1142 VU0071063 ≥98% (HPLC) VU0071063 is a potent activator of Kir6.2/SUR1 KATP channels (EC50 = 10.3 μM). VU0071063 reversibly inhibits glucose-stimulated calcium influx in mouse β-islet cells. The compound VU0071063 has no affect on Kir6.2/SUR2A channels.
VU0071063 is also known as [7-(4-(tert-butyl)benzyl)-1,3-dimethyl-1H-purine-2,6(3H,7H)-dione]. It serves as a major compound for examining β-cell physiology, KATP channel gating and a new chemical scaffold for evolving enhanced activators with medicinal chemistry.
SML2431 VU0134992 hydrochloride ≥98% (HPLC) VU0134992 is an orally available, potent and selective modulator of the inward rectifier potassium (Kir) channel Kir4.1 (KCNJ10) that induces diuresis, natriuresis, and kaliuresis in rats.
V5015 VU0152100 ≥98% (HPLC) Positive allosteric modulator of muscarinic choline receptor M4. Potentiates activation by acetylcholine, but posesses no intrinsic agonist activity alone.
V1640 VU0155041 ≥98% (HPLC) VU0155041 is a mixed allosteric agonist/positive allosteric modulator (PAM) of mGluR4. VU0155041 is approximately 8-fold more potent than PHCCC and does not show any significant potentiator or antagonist activity at other mGluR subtypes. It is soluble in an aqueous vehicle and intracerebroventricular administration of 31-316 nmol of VU0155041 dose-dependently decreased haloperidol-induced catalepsy and reserpine-induced akinesia in rats. VU0155041 exhibits selectivity for mGluR4 relative to 67 different targets and does not affect the function of striatal NMDA receptors.
VU0155041 is a positive allosteric modulator of the metabotropic glutamate receptor subtype 4. It also shows some direct agonist activity, but at a site different from the glutamate binding site. /VU0155041 is approximately 8-fold more potent than PHCCC and enhances the activity of glutamate also about 8-fold. It shows promising anti-Parkinsonian effects in animal models of Parkinson′s disease.
SML2279 VU0155069 ≥98% (HPLC) VU0155069 is a PLD1-selective catalytic site-targeting phospholipase D inhibitor (PLD1/2 IC50 = 46 nM/933 nM by cell-free enzymatic assays; substrate = di-palmitoyl-PLC) that selectively suppresses the cellular PLD activity in PMA-stimulated non-small-cell lung cancer (NSCLC) Calu-1 cells with predominant PLD1 activity over GFP-PLD2-overexpressing HEK293 cells (IC50 = 11 nM and 1.8 μM, respectively). Note: VU0155069 is reported to impair P2X7-induced pore formation in human RPMI 8226 B cells lacking PLD1 expression.
SML2714 VU0155072 ≥98% (HPLC) VU0155072 is a PLD2-selective, PH domain-targeting allosteric phospholipase D inhibitor (human PLD2/PLD1 IC50 = 140 nM/5.1 μM vs. PH/PX-deleted rat PLD1 IC50 >20 μM; cellular PLD IC50 = 110 nM/GFP-PLD2-overexpressing HEK293 vs. 1 μM/PMA-stimulated Calu-1 with predominant PLD1 activity) that selectively suppresses PLD2-dependent MDA-MB-231 invasion in cultures (by 60% in 48 hrs; 200 nM) and exhibits in vivo efficacy in murine models of DSS-induced colitis (4 mg/kg/day p.o.) and breast tumor-associated macrophages/neutrophils infiltration (75 μg/0.11 μL/kg/hr via osmotic pump). Use low concentrations (<5 μM) for cell treatment to avoid dual PLD1/2 inhibition.
V4515 VU0238429 solubility: ≥20 mg/mL in DMSO VU0238429 is a selective muscarinic acetylcholine receptor 5 (M5) positive allosteric modulator; causes leftward shift in acetylcholine potency. M5 is thought to regulate cerebral blood flow, and activation of M5 may be therapeutic for Alzheimer′s disease. VU0238429 is the first reported M5-selective small molecule of any kind. It is >30-fold more selective for M5 over M1, M2, M3, and M4.
V3890 VU0240551 ≥98% (HPLC) VU0240551 is a potent, selective KCC2 inhibitor. KCC2 is a potassium-chloride exchanger expressed specifically in neurons. KCC2 functions to lower intracellular chloride concentrations below the electrochemical potential of the cells, thereby increasing the hyperexcitability of the neurons. KCC2 activity enhances GABA and other inhibitory neurotransmission and is implicated in pain processing. VU0240551 was discovered in a high-throughput screen, followed by directed medicinal chemistry. VU0240551 is selective for KCC2 over NKCC1. VU0240551 binds competitively to the K+ site and binds noncompetitively to the Cl- site. VU0240551 is the only small molecule with specificity for a KCC family member.
V3765 VU0255035 hydrate ≥98% (HPLC) VU0255035 is the first highly selective antagonist at the orthosteric site of the M1 receptor (75-fold selective for M1 relative to other muscarininc subtypes and devoid of activity at other GPCRs, ion channels, transporters and kinases). There are no highly selective M1 muscarinic receptor antagonists. The existing non-selective drugs do not permit direct evaluation of the role of M1 receptors in CNS fucntions and do not premit therapeutic targeting of M1 receptors in various disease states in which M1 receptors are implicated (epilepsy, Parkinson′s disease, attention and cognitive disorders, dystonia, etc).
V4640 VU0357017 monohydrochloride ≥98% (HPLC) VU0357017 is a subtype-selective M1 muscarinic acetylcholine allosteric agonist. VU0357017 has a potency of 200 nM and Achmax of 81% and had no activity at M2-M5 up to the highest concentrations tested and also had little or no detectable antagonist activity at any other mAChR subtype at concentrations over 2 orders of magnitude higher than those required to activate M1 or activity at a large panel of GPCRs, ion channels, and transporters. In contrast, TBPB inhibited responses to ACh at each of the other mAChR subtypes. VU0357017 was active in reversing cognitive deficits induced by scopolamine in a preclinical rodent model.
SML0019 VU0357121 ≥98% (HPLC) VU0357121 is a positive allosteric modulator (PAM) of the metabotropic glutamate receptor 5 (mGlu5) with EC50 = 33 nM, 92% Glumax. Its site of action is distinct from the classical mGlu5 negative allosteric modulator (NAM) MPEP allosteric site or the site of a recetly discovered PAM, CPPHA. However, VU0357121shares a functional interaction with the MPEP site. VU0357121 is highly selective for activation of mGlu5 and is inactive or very weakly antagonizing at other mGlu receptor subtypes.
SML0494 VU0361737 ≥98% (HPLC) VU0361737 is an mGluR4-specific positive allosteric modulator (PAM) with greater than 50 fold selectivity over other mGluR subtypes. The EC50 values for human and rat mGlu4 are 240 and 110 nM, respectively, compared to greater than 10 mM for all other mGluRs.
SML0672 VU0405601 ≥98% (HPLC) VU0405601 is a hERG (the human Ether-à-go-go-Related Gene) agonist that increased the IC50 of dofetilide from 38.7 nM to 76.3 nM. VU0405601 protects against arrhythmias induced by hERG inhibition.
SML2783 VU0409551 ≥98% (HPLC) VU0409551 (JNJ-46778212) is an orally available, potent and selective biased metabotropic glutamate receptor subtype 5 positive allosteric modulator (mGlu5 PAM). VU0409551 (JNJ-46778212) selectively potentiates mGlu5 coupling to Gaq-mediated signaling without modulation of NMDAR currents in hippocampal neurons. VU0409551 exhibits potent antipsychotic-like and cognition enhancing activity in animal models.
SML2831 VU041 ≥98% (HPLC) VU041 is a mosquito cuticle penetrant, potent and selective inhibitor of inwardly rectifying potassium (Kir) channel of Aedes aegypti (AeKir1) and Anopheles gambiae (AnKir1) that exhibits potent toxicity to adult insecticide-susceptible and -resistant strains of female mosquitoes. VU041 is selective for mosquito Kir channels over several mammalian orthologs. Also, VU041 is toxic to mosquito larvae when present in water.
SML1357 VU0453379 hydrochloride ≥98% (HPLC) VU0453379 is a highly selective CNS penetrant positive allosteric modulator of Glucagon-like peptide-1 (GLP-1) with GLP-1 EC50 = 1.3 μ,M, 59.2% GLP-1 max. VU0453379 potentiated low-dose exenatide to augment insulin secretion in primary mouse pancreatic islets. In a model of Parkinson’s disease it showed a significant reversal of haloperidol-induced catalepsy at 30 mg/kg.
SML2333 VU0463271 ≥98% (HPLC) VU0463271 is a potent and selective potassium-chloride cotransporter 2 (KCC2) inhibitor that displays greatly enhanced potency than its structural analogs VU0255011 (ML077) & VU0240511 (IC50 = 61, 537, and 568 nM, respectively). VU0463271 exhibits much reduced efficacy against the related Na-K-2Cl cotransporter 1 (NKCC1 inhibition max ~37% at 100 μM) and little affinity toward a panel of 68 GPCRs, ion channels, and transporters. Although VU0463271 is reported to exhibit affinity toward mitochondrial translocator protein TSPO (IC50 of 204 nM against PK11195 binding; rat heart) and inhibitory potency against α1B adrenergic receptor (IC50 of 364.7 nM; human α1B CHO transfectants), these proteins are not known to affect chloride homeostasis.
SML0077 VU591 ≥98% (HPLC) VU591 is a Potassium Inwardly-Rectifying Channel (KCNJ1 or ROMK) specific inhibitor (IC50 = 240 nM) that is closely related to VU590. Unlike VU590, VU591 does not inhibit Kir7.1. The compound has a modest effect on Kir6.2/SUR1, causing 17% inhibition at 10 uM.
human ... KCNJ1(3758)
SML1336 VUAA1 ≥98% (HPLC) N-(4-ethylphenyl)-2-((4-ethyl-5-(3-pyridinyl)-4H-1,2,4-triazol-3-yl) thio) acetamide (VUAA1) is a non-naturally occurring volatile compound. It is considered as a valuable tool for insect olfactory research.
VUAA1 is an agonist of the highly conserved insect odorant receptor co-receptor ion channel Orco. VUAA1 is able to activate both heteromeric and homomeric Orco-containing channels, acting as an insect repellant by over-activating an insect′s olfactory senses causing a repellent effect.
SML0803   VUF10661 ≥98% (HPLC) VUF10661 is a potent agonist of the chemokine receptor CXCR3. VUF10661 induces receptor internalization, recruitment of ?-arrestins and activates Gi proteins with similar potency to endogenous CXCL ligands.
SML0669 VUF11207 trifluoroacetate salt ≥98% (HPLC) VUF11207 is a highly potent CXCR7 agonist. VUF11207 induces recruitment of β-arrestin2 to the CXCR7 followed by internalization of the receptor.
VUF11207 is considered as a selective inhibitor of CXCR4 (C-X-C motif chemokine receptor 4).
V5888 VUF 5574 Potent, selective, and competitive A3 adenosine receptor antagonist.
human ... ADORA3(140)
V4390 VUF 8430 dihydrobromide ≥97% (NMR) VUF 8430 dihydrobromide is a potent histamine H4 receptor agonist, with a 33-fold selectivity over the histamine H3 receptor and negligible affinity for the other histamine receptor.
SML2158 VX-680 ≥98% (HPLC) VX-680 is an ATP site-targeting potent aurora kinase inhibitor (Aurara A/B/C Ki(app) = 0.6/18/4.6 nM) that affects FLT3, BCR-Abl, BCR-Abl (T315I), Lck, ITK, Src, and Fyn only at higher concentrations (Ki(app) = 30, 30, 42, 80, 220, 350, 520 nM, respectively) and exhibits little inhibitory potency toward 52 other kinases (Ki(app) >1 μM). VX-680 exhibits potent antiproliferation activity in a wide variety of cancer cultures (IC50 from 15 to 113 nM) as a result of cell cycle arrest and apoptosis induction, as well as causes tumor retardation (by 98% on day 13; 75 mg/kg b.i.d i.p.; HL-60 in mice) and regression (2 mg/kg/h 3 d/wk i.v. infusion; HCT116 in rats) in vivo. Crystallography data reveal a tight association of VX-680 with a hydrophobic pocket present only in a closed, inactive kinase conformation, which forms the basis of its selectivity profile, including its activity toward wild-type and the Imatinib-resistant (T315I) Abl.
SML2493 VX-702 ≥98% (HPLC) VX-702 is a second generation p38α MAPK inhibitor with 14-fold higher potency against p38α versus p38β.
SML1638 VX-745 ≥98% (HPLC) VX-745 is a selective blood-brain barrier penetrant inhibitor of p38 MAPKα. VX-745 showed 20-fold selectivity for p38α over p38β and a Ki value of 220 nM. VX-745 has been shown to reduce inflammation in an arthritic (AIA) mouse model and to improve performance in aged rats.
human ... MAPK14(1432)