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SML0089 Abacavir sulfate ≥98% (HPLC) Abacavir incorporated in the cells is converted to triphosphate containing guanine analog carbovir (CBV) and it favors the generation of higher double stranded breaks (DSBs).
Abacavir sulfate is a Nucleoside analog reverse transcriptase inhibitor (NRTI); guanosine analog used to treat HIV and AIDS.
A4669 Acycloguanosine ≥99% (HPLC), powder Antiviral agent. Phosphorylation by herpes simplex virus thymidine kinase (HSV-TK) leads to the formation of acycloguanosine triphosphate that competitively inhibits the viral DNA polymerase.
Antiviral agent. Phosphorylation by herpes simplex virus thymidine kinase (HSV-TK) leads to the formation of acycloguanosine triphosphate that competitively inhibits the viral DNA polymerase. Acycloguanosine can be used to induce apoptosis in cells transfected with HSV-TK. Inhibits replication of cytomegalovirus by a mechanism that is independent of its phosphorylation by viral or cellular thymidine kinase.
human ... HV1S(3365), NP(4860)
A3477 AH 11110 >98% (HPLC), solid α1B-adrenoceptor ligand
A9102 AH13205 ≥98% (HPLC), oil AH13205 is a selective, low potency agonist for the EP2 receptor. AH13205 has been shown to compete with Prostaglandin E2 (PGE2) for binding, resulting in the displacement of PGE2 binding.
A8227 AH23848 hemicalcium salt ≥90% (HPLC), powder AH23848 regulates nitric oxide (NO) production and reduces endogenous cAMP accumulation. This is carried out by declination of inducible nitric oxide synthase (iNOS) gene expression and acceleration of iNOS protein degradation in glomerular mesangial cells.
EP4 prostanoid receptor antagonist with TP blocking activity.
A7986 Atovaquone ≥98% (HPLC) Atovaquone is an anti-protozoal mitochondrial electron transport inhibitor; Antimalarial; Antipneumocystic, and has also been used to treat toxoplasmosis. It is an analog of protozoan mitochondrial protein ubiquinone, and acts by inhibiting the cytochrome bc(1) complex via interactions with the Rieske iron-sulfur protein and cytochrome b in the ubiquinol oxidation pocket.
B0385 Beclomethasone ≥99% Beclomethasone is an anti-inflammatory glucocorticoid.
It helps to decrease airway hyperresponsiveness. It also helps to regulate symptoms of asthma.
human ... CYP1A2(1544)
B4559 BRL 44408 maleate salt ≥98% (HPLC) BRL 44408 maleate is a selective α2A-adrenoceptor antagonist.
B0936 BRL 50481 ≥98% (HPLC), solid BRL 50481 is a potent and selective PDE7 inhibitor (IC50 = 260 nM).
human ... PDE7A(5150), PDE7B(27115)
B102 Bupropion hydrochloride ≥98% (HPLC), solid Bupropion possesses antidepressant and anxiolytic properties. It serves as a good auxiliary for people who makes an effort to give up smoking. It may also be used in the treatment for attention-deficit hyperactivity disorder.
Inhibits the dopamine and norepinephrine transporters with Kis of 2.8 μM and 1.4 μM, respectively. Does not inhibit the serotonin transporter (Ki = 45 μM). Antidepressant.
human ... DRD1(1812), DRD2(1813), DRD3(1814), DRD4(1815), DRD5(1816), SLC6A2(6530), SLC6A3(6531)
C3993 Carvedilol ≥98% (HPLC), solid Cavedilol is a non-selective β-adrenergic blocker with α1 blocking activity. Carvedilol is used specifically for the treatment of heart failure and high blood pressure. It has been shown to improve left ventricular ejection fraction and may reduce mortality.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146), ADRB1(153), ADRB2(154), ADRB3(155)
C8138 Chlorpromazine hydrochloride ≥98% (TLC) Chlorpromazine demonstrates cytotoxic and antiproliferative activity against leukemic cells, but does not affect the viability of normal lymphocytes.
Phenothiazine antipsychotic; D2 dopamine receptor antagonist, H1 histamine receptor antagonist; inhibits calmodulin-dependent stimulation of cyclic nucleotide phosphodiesterase and nitric oxide synthase.
human ... DRD2(1813), DRD3(1814), DRD4(1815), HRH1(3269), HTR2A(3356)
C4522 Cimetidine H2 histamine receptor antagonist; I1 imidazoline receptor agonist; anti-ulcer agent. Blocks cancer metastasis by inhibiting the expression of E-selectin on the surface of endothelial cells, thus blocking tumor cell adhesion.
human ... ABCB1(5243), CYP1A2(1544), CYP3A4(1576), HRH2(3274), SLC9A2(6549), SLC9A5(6553)
mouse ... Abcb1a(18671), Abcb1b(18669)
rat ... Slc9a1(24782), Slc9a3(24784), Slc9a5(192215)
D5321 D36 hydrate ≥98% (HPLC) D36 is an androgen receptor (AR) allosteric antagonist with inverse agonist properties. D36 inhibits both wild-type and agonist-induced AR activity and antagonized AR in a hormone-refractory model.
D1944 D4476 ≥98% (HPLC), solid D4476 is a potent, selective ATP-competitive inhibitor of CK1 (casein kinase 1).
D4476 may prevent or enhance apoptosis. It triggers tumor suppressor p53 and impairs transcription factor E2F-1.
D1260 Decamethonium bromide crystalline Decamethonium serves as a muscle relaxant and is also a neuromuscular blocking agent. It has a molecular weight of 258.4.
Nicotinic acetylcholine receptor partial agonist and neuromuscular blocking agent; depolarizes striated muscles and blocks their activity.
human ... CHRNA1(1134), CHRNA10(57053), CHRNA2(1135), CHRNA3(1136), CHRNA4(1137), CHRNA5(1138), CHRNA6(8973), CHRNA7(1139), CHRNA9(55584), CHRNB1(1140), CHRNB2(1141), CHRNB3(1142), CHRNB4(1143), CHRND(1144), CHRNE(1145), CHRNG(1146)
E2535 Eprosartan mesylate ≥98% (HPLC) Angiotensin II type 1 (AT1) receptor antagonist; anti-hypertensive.
human ... AGTR1(185)
F9428 Fluticasone propionate ≥98% (HPLC), powder Fluticasone propionate is a second generation glucocorticoid. Used as an anti-inflammatory agent for asthma. Shown to enhance eosinophil apoptosis in a concentration-dependent manner via the glucocorticoid receptor.
human ... NR3C1(2908)
G0544 GR 103691 ≥98% (HPLC), solid D3 dopamine receptor antagonist.
rat ... Htr1a(24473)
G5918 GR 113808 ≥98% (HPLC), solid GR 113808 is a 5-HT4 serotonin receptor antagonist.
human ... HTR4(3360)
rat ... Htr3a(79246), Htr4(25324)
G5793 GR 127935 hydrochloride hydrate >98% (HPLC), powder Potent, selective and orally active 5-HT1B/1D serotonin receptor antagonist.
human ... HTR1B(3351), HTR1D(3352)
G5044 GR 32191B ≥98% (HPLC), solid Selective TP prostanoid receptor antagonist. Inhibits U-46619-induced contraction of guinea pig trachea with IC50=1.8 nM.
G5797 GSK0660 ≥98% (HPLC) GSK0660 is a potent PPARβ/δ antagonist with a pIC50 of 6.8 (160 nM). GSK0660 is nearly inactive on PPARα and PPARγ with IC50s greater than 10 μM.
G0798 GSK1016790A ≥98% (HPLC) GSK1016790A is a novel and potent TRPV4 channel agonist. The TRPV4 (transient receptor potential vanilloid 4) member of the TRP superfamily has been implicated in numerous physiological processes. GSK1016790A elicited Ca2+ influx in mouse and human TRPV4 expressing HEK cells (EC50 values of 18 and 2.1 nM, respectively), and evoked a dose-dependent activation of TRPV4 whole-cell currents at concentrations above 1 nM. It is 300 fold more potent than 4a-PDD (Cat. No. P8014).
SML0083 GSK 1059615 sodium salt hydrate GSK 1059615 is a phosphatidylinositol-3-kinases (PI3K) inhibitor. GSK 1059615 inhibits proliferation of breast cancer BT474 cells via four different mechanisms that include retinoblastoma 1 (RB1)-mediated cell cycle arrest, elevated forkhead box protein O1 (FOXO) signaling, deduced MYC and transferrin receptor (TFRC) signaling and decreased cellular metabolism. Additionally, GSK 1059615 can suppress cell proliferation by decreasing mitogen-activated protein kinase (MAPK) signaling and imparts sensitivity to phosphoinositide 3-kinase (PI3K) inhibitor in cells resistant to the protein kinase B or AKT inhibitor. GSK 1059615 functions as a druggable target to reduce radiation-induced apoptosis in NCCIT cells. GSK 1059615 has entered clinical trial in patients with solid tumors or lymphoma and refractory malignancies.
GSK 1059615 is a potent inhibitor of PI3 Kinase. (IC50 = 2 nM)
G7423 GSK3787 ≥98% (HPLC), white to off-white, powder GSK3787 is an orally available selective irreversible Peroxisome Proliferator-Activated Receptor δ (PPARδ) antagonist (pIC50=6.6) with no measurable affinity for hPPARR or hPPARγ (pIC50<5). It acts by covalently modifying Cys249 within the ligand binding pocket, and has been shown to antagonize the induction of PPARδ-regulated target genes in skeletal muscle cells.
G0673 GSK4112 ≥98% (HPLC) GSK4112 is a rev-erbα, (orphan nuclear receptor NR1D1) agonist, the first agent able to reset the circadian clock in a phase-dependent manner. Rev-erbα impacts the precision of the circadian clock by repressing target gene activities with the help of a nuclear receptor co-repressor complex (NCoR) and HDAC3. GSK4112 competes with heme (rev-erb′s natural ligand) and enhances co-repressor complex recruitment and thus, repression of transcription. suggests that pharmacological modulation through Rev-erb may provide new routes to treat metabolic diseases, especially disorders of adipogenesis regulated by rev-erba.
G6173 GSK 4716 ≥98% (HPLC) GSK 4716 is an Estrogen-related receptors ERRβ and ERRγ agonist with minimal activity for ERRα, ERα and ERβ
G5547   GSK837149A ≥98% (HPLC), solid GSK837149A is the first selective inhibitor of human fatty acid synthase (FAS) known to act specifically and selectively on the KR activity of the enzyme. It was first isolated as a minor impurity in a sample found to be active against the enzyme in a high-throughput screening campaign. This compound and its analogs synthesized, all being symmetrical structures containing a bisulfonamide urea, act by inhibiting the beta-ketoacyl reductase activity of the enzyme. GSK837149A inhibits FAS in a reversible mode, with a Ki value of approximately 30 nm, and it possibly binds to the enzyme-ketoacyl-ACP complex. Although initial results suggest that cell penetration for these compounds is impaired, they still can be regarded as useful tools with which to probe and explore the beta-ketoacyl reductase active site in FAS, helping in the design of new inhibitors.
G3295 GW0742 ≥98% (HPLC) GW0742 is a highly selective PPARδ agonist. EC50 = 1 nM vs 1 μM and 2 μM for PPARα and PPARγ, respectively.
human ... PPARA(5465), PPARD(5467), PPARG(5468)
G5668 GW1929 hydrate >98% (HPLC), solid GW1929 is a high affinity agonist of PPAR-γ.
human ... PPARG(5468)
G0668 GW2974 ≥98% (HPLC), solid Potent and selective dual inhibitor of EGFR (IC50 = 0.016 mM) and ErbB-2 receptor tyrosine kinase.
human ... EGFR(1956), ERBB2(2064)
G6295 GW3965 hydrochloride ≥98% (HPLC), powder GW3965 is a liver X receptor full agonist on hLXRα and hLXRβ. GW3965 has an EC50 = 125 nM in a cell-free ligand-sensing assay of LXRα and profiles as a full agonist on hLXRα and hLXRβ in cell-based assays with EC50 = 190 nM and 30 nM, respectively. It is orally active in mice. When screened against a panel of nuclear receptors, it cross-reacted with only the pregnane X receptor (PXR). The literature agonist, T0901317 (Tularik), had an EC50 = 60 nM and 85 nM in the cell-free and cell-based assays, respectively.
G5172 GW4064 ≥97% (HPLC) GW4064 is a FXR agonist. GW4064 is a potent (EC50 = 15 nM), non-steroidal agonist of the orphan nuclear receptor FXR. It shows no activity on other nuclear receptors including RAR up to 1 mM. This is an important tool for the study of the involvment of FXR in a variety of biological activities.
D1692 GW4869 ≥90% (NMR) A cell-permeable, potent, specific, non-competitive inhibitor of N-SMase (neutral sphingomyelinase)
G3545 GW583340 dihydrochloride ≥97% (HPLC), solid Potent dual ErbB-2/EGFR tyrosine kinase inhibitor. IC50= 0.01 and 0.014 μM for EGFR and ErbB-2. Orally active.
G5045 GW6471 ≥98% (HPLC) GW6471 is a PPARα antagonist, which completely inhibits GW409544-induced activation of PPARα with an IC50 = 0.24 μM. GW6471 induces a PPARα conformation that interacts efficiently with co-repressors.
SML0116 GW788388 Hydrate ≥98% (HPLC) GW788388 is a potent selective inhibitor of TGF-beta type I receptor [activin receptor-like kinase 5 (ALK5)]. GW788388 is orally available with a half-life of approximately 4 hours.
SML0230   GW-803430 ≥98% (HPLC) GW-803430 antagonizes central MCHR1 and produces anxiolytic, anti-depressant and anti-obesity effects in rats and mice. It also controls the alcohol-seeking behavior in rats and is a promising treatment for alcohol use-related disorders.
GW-803430 is a centraly active and selective melanin-concentrating hormone receptor (MCHR) 1 antagonist
G2171 GW843682X ≥98% (HPLC), solid GW843682X is a polo-like kinase-1 (PLK1) and polo-like kinase-3 (PLK3) inhibitor with nanomolar activity. It shows potent inhibition of proliferation of a wide variety of tumor cell lines.
H9414 Halofantrine hydrochloride ≥98% (HPLC), solid Halofantrine is a blocker of delayed rectifier potassium current via the inhibition of hERG channel.
K2144 Ko143 hydrate ≥98% (HPLC) Ko143 has been used as a positive control inhibitor on functions of BCRP in MCF7 and BCRP over-expressing MCF7/MX100 cell lines using a BCRP prototypical substrate mitoxantrone. The ABCG2 transporter breast cancer resistance protein (BCRP) plays an important role in disposition of many drugs and environmental toxins. Ko143 displays > 200-fold selectivity over P-gp and MRP-1 transporters. It increases intracellular drug accumulation and reverse BCRP-mediated multidrug resistance. It blocked topotecan and ABZSO transport in a concentration-dependent manner. Ko143 is reported to be a more specific inhibitor of BCRP than other known inhibitors of BCRP such as fumitremorgin C and GF120918.
Ko143 has been used as a positive control inhibitor on functions of breast cancer resistance protein (BCRP) using a BCRP prototypical substrate mitoxantrone. BCRP, an ABCG2 transporter, plays an important role in disposition of many drugs and environmental toxins. Ko143 displays > 200-fold selectivity over P-gp and MRP-1 transporters and thus is more specific than other known BCRP inhibitors such as fumitremorgin C and GF120918. It increases intracellular drug accumulation and reverses BCRP-mediated multidrug resistance. It blocks topotecan and ABZSO transport in a concentration-dependent manner.
L2167 L-165,041 ≥98% (HPLC), powder PPARβ (PPARδ) selective agonist.
human ... PPARD(5467)
L1295 Lamivudine ≥98% (HPLC), powder Lamivudine is a potent nucleoside analog reverse transcriptase inhibitor (nRTI). It is an analogue of cytidine, and can inhibit both types (1 and 2) of HIV reverse transcriptase as well as the reverse transcriptase of hepatitis B. It needs to be phosphorylated to its triphosphate form before it is active. 3TC-triphosphate also inhibits cellular DNA polymerase.
L3791 Lamotrigine ≥98%, powder Anticonvulsant.
human ... SCN10A(6336), SCN11A(11280), SCN1A(6323), SCN2A(6326), SCN3A(6328), SCN4A(6329), SCN5A(6331), SCN7A(6332), SCN8A(6334), SCN9A(6335)
rat ... Scn2a1(24766), Scnn1a(25122)
M7694 Mupirocin ≥92% (HPLC), powder Antibiotic; inhibits isoleucyl-tRNA synthetase (IRS).
N1415 Naratriptan hydrochloride ≥98% (HPLC) Naratriptan hydrochloride is a serotonin 5-HT1B/1D receptor agonist.
human ... HTR1B(3351), HTR1D(3352)
O3639 Ondansetron hydrochloride dihydrate ≥98% (HPLC), powder 5-HT3 serotonin receptor antagonist
Ondansetron, (3RS)-9-methyl-3-[(2-methyl-1H-imidazol-1-yl) methyl] 1,2,3,9-tetrahydro-4H-carbazol-4-one hydrochloride dehydrate acts as a selective 5-hydroxytryptamine type 3 (5-HT3) serotonin receptor antagonist. It is used as an antiemetic to control nausea and vomiting associated with chemotherapy and radiotherapy.
human ... HTR3A(3359)
P9623 Paroxetine hydrochloride hemihydrate ≥98% (HPLC), powder Paroxetine hydrochloride hemihydrate is one of the most potent and selective of the selective serotonin reuptake inhibitors (SSRI); antidepressant
Paroxetine is a phenylpiperidine derivative. It has the ability to cross placenta. Paroxetine is known to increase the risk of congenital cardiac malformations. It might be useful in hormone replacement therapy for treating vasomotor symptoms during menopause. It is known to ameliorate the effects of panic disorder, obsessive‐compulsive disorder and social phobia.
human ... SLC6A4(6532)
P1372 Paroxetine maleate salt ≥98% (HPLC), solid Paroxetine is a strong cytochrome P450 2D6 isotype (CYP2D6) inhibitor, which reduces the effectiveness of tamoxifen. This phenylpiperidine derivative inhibits clozapine metabolism. Paroxetine is used to treat social phobia, obsessive-compulsive disorder and panic disorder. It is also used to treat the premenstrual dysphoric disorder, post-traumatic stress disorder and chronic headache.
Paroxetine maleate is a selective serotonin reuptake inhibitor; antidepressant.
human ... SLC6A4(6532)
P9248 PD 169316 ≥98% (HPLC), solid Potent, cell-permeable and selective p38 MAP kinase inhibitor (IC50 = 89 nM).
human ... MAPK14(1432)
P9178 Prochlorperazine dimaleate salt Phenothiazine antipsychotic; D2 dopamine receptor antagonist; antispasmodic
Prochlorperazine is an anti-nausea and neuroleptic agent. It is known to cause neuropsychiatric side effects. Prochlorperazine inhibits the action of dopamine in the central nervous system. It acts as an antiemetic drug and prevents vomiting and stimulates sleep. Prochlorperazine is useful as a tranquilizer in the treatment of schizophrenia and nonpsychotic anxiety.
human ... DRD2(1813)
P4670 Propafenone hydrochloride Blocks hKv1.5 and ATP-sensitive K+ channels; class 1C antiarrhythmic agent that is also an antagonist at β adrenergic receptors.
human ... ABCB1(5243), ADRB1(153), ADRB2(154), ADRB3(155), CYP1A2(1544), SCN10A(6336), SCN11A(11280), SCN1A(6323), SCN2A(6326), SCN3A(6328), SCN4A(6329), SCN5A(6331), SCN7A(6332), SCN8A(6334), SCN9A(6335)
R101 Ranitidine hydrochloride solid H2 histamine receptor antagonist; anti-ulcer agent.
Ranitidine is mainly used to treat gastrointestinal impairment instigated by non-steroidal anti-inflammatory drugs (NSAIDs).
human ... HRH2(3274)
R2530 Ropinirole hydrochloride powder, ≥98% (HPLC) An agonist at the D2 and D3 dopamine receptor subtypes, binding with higher affinity to D3 than to D2 or D4. It has negligible effect on D1-receptors. It has medium in vitro affinity to opioid receptors. Ropinirole is said to have virtually no affinity to 5-HT1, 5-HT2, benzodiazepine, GABA, muscarinic, α1-, α2-, and β-adrenoreceptors. Used as antiparkinsonian drug.
Ropinirole hydrochloride is effectively used to treat early and late Parkinson′s disease.
human ... DRD2(1813), DRD3(1814), DRD4(1815)
R2408 Rosiglitazone ≥98% (HPLC) Rosiglitazone is a potent agonist for PPARγ with an EC50 of 43 nM for the human receptor. It is antidiabetic, working as an insulin sensitizer by binding to the PPARγ receptors in fat cells and making the cells more responsive to insulin.
human ... PPARG(5468)
S8260 Salbutamol β2-adrenoceptor agonist
Salbutamol is a β2 adrenoceptor agonist with short acting bronchodilation and anti-inflammatory effects. It relaxes the airway smooth muscles and inhibits bronchoconstriction induced by adenosine-5′ -monophosphate (AMP).1 Salbutamol is particularly effective in treatment of asthma as it provides immediate relief.2
human ... ADRB2(154)
S5013 Salbutamol hemisulfate salt ≥98% β2-Adrenergic receptor agonist.
Salbutamol is a β2 adrenoceptor agonist with short acting bronchodilation and anti-inflammatory effects. It relaxes the airway smooth muscles and inhibits bronchoconstriction induced by adenosine-5′ -monophosphate (AMP).1 Salbutamol is particularly effective in treatment of asthma as it provides immediate relief.2
Salbutamol is a β2 adrenoceptor agonist with short acting bronchodilation and anti-inflammatory effects. It relaxes the airway smooth muscles and inhibits bronchoconstriction induced by adenosine-5′ -monophosphate (AMP). Salbutamol is particularly effective in treatment of asthma as it provides immediate relief. Salbutamol is one of the most popular short-acting BA (SABA). It is useful in treating the symptoms of EIB (exercise induced bronchospasm).
human ... ADRB2(154)
S5068   Salmeterol xinafoate ≥98% (HPLC), solid β2-adrenoceptor agonist.
Salmeterol xinafoate is a β2 adrenoceptor agonist with longer lasting bronchodilation and anti-inflammatory effects. It relaxes the airway smooth muscles, stabilizes mast cells and regulates the release of histamine. Salmetrol is particularly effective in treatment of mild asthma, chronic obstructive pulmonary disorder.5,6
human ... ADRB2(154)
S7067 SB 202190 ≥98% (HPLC) SB 202190 is a highly selective, potent and cell permeable inhibitor of p38 MAP kinase. SB 202190 binds within the ATP pocket of the active kinase (Kd = 38 nM, as measured in recombinant human p38), and selectively inhibits the p38α and β isoforms.
human ... MAPK14(1432)
S7076 SB 202190 monohydrochloride hydrate ≥98% (HPLC) SB 202190 binds within the ATP pocket of p38 kinase and inhibits the p38α and β isoforms.
SB 202190 is a highly selective, potent, and cell-permeable inhibitor of p38 MAP kinase.
SB 202190 monohydrochloride hydrate mediates the phosphorylation of serine in the mutant p53 protein and modulates cell adhesion and prevents cell proliferation in breast cancer cell lines.
S0693 SB 204741 >98% (HPLC) 5-HT2B serotonin receptor antagonist.
human ... DRD2(1813), DRD3(1814), DRD5(1816), HTR1E(3354), HTR2A(3356), HTR2B(3357), HTR2C(3358)
rat ... Adra1a(29412), Gabra2(29706), Htr1a(24473), Htr2b(29581), Htr3a(79246)
S1068 SB-215505 solid, >98% (HPLC) Selective 5-HT2B serotonin receptor antagonist; 100-fold higher affinity at 2B versus 2C.
human ... HTR2B(3357)
S3442 SB 216763 >98% (HPLC) Potent, selective, cell permeable glycogen synthase kinase-3 (GSK-3) inhibitor.
SB-216763 is a small molecule that competes with ATP and potently inhibits the activity α and β isozymes of GSK-3. It acts as neuroprotectant and prevents neuronal cell death induced by PI3-kinase pathway. It also delays preconditioning, reduces infarct size and prevents cardiac ischemia.
human ... GSK3A(2931), GSK3B(2932)
S9070 SB 220025 trihydrochloride ≥98% (HPLC), solid SB 220025 is a potent, specific inhibitor of human p38 mitogen-activated protein (MAP) kinase, with an IC50 value of 60 nM and 50- to 1000-fold selectivity. SB 220025 reduces inflammatory cytokine production and inhibits angiogenesis. SB 220025 reduced the lipopolysaccharide-induced production of TNF at an ED50 value of 7.5 mg/kg. At 30 mg/kg, SB 220025 reduced the expression of TNF and inhibited angiogenesis by ~40%. In a further study, the effects of p38/CSBP MAP kinase inhibition in angiogenesis-dependent chronic inflammatory disease was tested in murine collagen-induced arthritis and SB 220025 was able to prevent the progression of established arthritis.
S5192 SB 222200 ≥98% (HPLC), solid Non-peptide NK3 tachykinin receptor antagonist.
SB 222200 is a 2-phenyl-4-quinolinecarboxamides and a selective, reversible and competitive antagonist of human NK-3 receptor that effectively crosses the blood-brain barrier. It inhibits the NK-3 receptor-induced miosis or pupil constriction in conscious rabbits.1,2
human ... TACR2(6865), TACR3(6870)
S0569 SB 239063 >98% (HPLC) Potent p38 MAP kinase inhibitor. Selective for α and β. No activity against γ and δ isoforms.
S8061 SB 242084 dihydrochloride hydrate ≥98% (HPLC), powder SB 242084 is a potent and selective antagonist of 5-HT2C receptor. It increases the basal activity of dopaminergic neurons and affects the behavioral responses mediated by 5-HT2C such as mesolimbic neuron activity and food intake.3,4,5
S1194 SB-258585 dihydrochloride ≥98% (HPLC), powder 5-HT6 serotonin receptor antagonist.
S5326 SB-271046A ≥98% (HPLC) The first potent and selective 5-HT6 antagonist. Training in cognitive tasks, as well as administration SB-271046, induces an increase in pERK1/2 and pCREB1 levels, while CREB2 levels are significantly reduced; cognition-enhancing properties of SB-271046 are attributed to the effect on pERK1/2, not pCREB1/2. SB-271046 reverses MK-801-induced, but not scopolamine-induced, learning impairments. However, with coadministration of galanthamine, both types of learning impairments were ameliorated.
S4326 SB-277011-A hydrochloride hydrate ≥98% (HPLC) SB-277011-A is a potent, selective brain-penetrant D3 dopamine receptor antagonist; 80-100x selective for D3 over D2; pKi = 7.95 for hD3 receptor.
The D3 dopamine receptor antagonist, SB-277011-A inhibits the cocaine-seeking behavior and cocaine-enhances brain stimulation reward in in rats. It decreases drug-seeking behavior and may be useful in treatment of cocaine and methamphetamine addiction.
SML0207 SB 328437 ≥98% (HPLC) SB 328437 inhibits the recruitment and migration of eosinophils in allergen models of models. It suppresses the Th2-mediated eosinophil infiltration in the airways.
SB-328437 is a potent, selective CCR-3 antagonist (IC50 = 1.6 nM). The compound blockes CCR3 agonist-induced calcium mobilization in CCR3 expressing cells with the following IC50 values: eotaxin, 38 nM; eotaxin-2, 35 nM and MCP4, 20 nM.
S0441 SB-366791 ≥98% (HPLC), powder SB-366791 might exhibit analgesic properties on bone cancer-related pain behavior.
Vanilloid receptor-1 (TRPV1) antagonist.
human ... TRPV1(7442)
S2694 SB-408124 ≥98% (HPLC), solid SB 408124 is an OX1 orexin receptor antagonist.
SB-408124 blocks the orexin type 1 receptor that stimulates the production of stress hormone in hypothalamus. It blocks orexin A-induced increase in arterial pressure and elevation of heart rate in rats. SB-408124 modulates phrenic nerve activity that is important in respiration.
S3567 SB 415286 ≥98% (HPLC) Glycogen synthase kinase-3 (GSK-3) inhibitor.
SB 415286 is a small molecule inhibitor of GSK-3 in muscle and fat cells. SB 415286 induces activation of glycogen synthase and regulates the transport glucose. SB 415286 reduces the systemic inflammation induced by endotoxic shock in rat model of acute colitis. It increases the axonal growth and promotes the recovery of injured adult CNS neurons. SB 415289 is implicated in inducing chromosome instability when used as therapeutic agents.
human ... GSK3A(2931), GSK3B(2932)
S4317 SB 431542 hydrate ≥98% (HPLC), powder Potent and selective inhibitor of transforming growth factor-β superfamily type I activin receptor-like kinase (ALK) receptors.
SB-431542 inhibits the TGF-β-mediated activation of SMAD proteins, expression of collagen and fibronectin, cell proliferation and cell motility. It does not inhibit kinases that are activated in response to serum or stress such as ERK, p38 or JNK.
S4696 SB-505124 hydrochloride hydrate ≥98% (HPLC) SB-505124 is an inhibitor of activin receptor-like kinase (ALK) 5, also known as transforming growth factor-α type I receptor kinase, with an IC50 of 47 ± 5 nM.
SB-505124 selectively inhibits TGF-β type I receptors, activin receptor-like kinases (ALK) 4, 5 and 7. It inhibits ALK4-, 5- and 7-mediated activation of Smad2, Smad3 and MAPK pathway induced by TGF-β.1 SB-505124 inhibits the human fibroblast trans-differentiation induced by the co-culture with Esophageal squamous cell carcinoma.2
S8822 SB-525334 ≥98% (HPLC) SB-525334 blocks the activation of Smad2/3 induced by TGFβ1 in renal proximal tubule cells.4 The sensitivity of TGFβ1 is decreased by SB-525334 that benefits the pulmonary arterial hypertension condition by reversing the pulmonary arterial pressure.5 SB-525334 is reduces the tumor incidence and size of mesenchymal tumors such as uterine leiomyoma.6
SB-525334 is a potent activin receptor-like kinase (ALK5)/ type I TGFβ-receptor kinase inhibitor with IC50 = 14.3 nM.
S7326 SB 657510 ≥98% (HPLC) SB 657510 slows development of diabetes-associated atherosclerosis in mouse model of diabetes.1
SB-657510 is a selective urotensin-II (UT) receptor antagonist. Human urotensin-II (hU-II) is proposed to play a significant role in cardiorenal and metabolic disease states, including heart failure, atherosclerosis, hypertension.
S9066 SKF-89976A >98% (HPLC), solid GABA transporter type 1 (GAT-1) inhibitor that crosses the blood brain barrier.
SKF-89976A contains a cyclic amino acid with lipophilic moiety that enables the compound to cross the blood-brain barrier.1,2 It decreases the excitotoxic swelling of chick retina cells by blocking the glutamate-induced GABA release.3
human ... SLC6A1(6529), SLC6A11(6538), SLC6A12(6539)
rat ... Slc6a1(79212), Slc6a12(50676)
S4194 SR 12813 ≥98%, solid SR 12813 is a pregnane X receptor (PXR, NR 112) agonist; cholesterol lowering drug; HMGCoA reductase inhibitor.
SR-12813 is a 1,1-bisphosphonate ester that exhibits hypocholesterolemic activity. It decreases the biosynthesis of cholesterol by enhancing the degradation of HMG-CoA reductase.
S1198 Sumatriptan succinate ≥98% (HPLC), solid Sumatriptan succinate has the ability to constrict human cranial arteries. This 5-HT1 receptor agonist can be used to treat migraine.
Sumatriptan succinate is a 5-HT1 serotonin receptor agonist.
human ... HTR1B(3351), HTR1D(3352)
T2705 Topotecan hydrochloride hydrate ≥98% (HPLC and enzymatic) Topotecan is a topoisomerase I inhibitor and an apoptosis inducer. It is a potent antineoplastic agent.
human ... TOP1MT(116447)
T1452 TPCA-1 ≥95% (HPLC) TPCA-1 is a potent and selective inhibitor of human IκB kinase-2 (IKK-2) with IC50 = 17.9 nM for IKK-2 compared to 400nm for IKK-1. It has been used to study inhibition of IKK-2 to prevent inflammatory mediator release in animal models of arthritis and airway inflammation.
T6764 Triprolidine hydrochloride ≥99% H1 histamine receptor antagonist.
human ... HRH1(3269)
W4262 1400W dihydrochloride >98%, solid 1400W dihydrochloride is a potent and selective inhibitor of inducible nitric oxide synthase (iNOS).
human ... NOS1(4842), NOS2(4843), NOS3(4846)