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L4795 L-365260 ≥98% (HPLC) L-365260 is a CCK2 selective antagonist. Enhances amphetamine-induced stimulation of locomotor activity in rats (a model of drug abuse), inhibits thyroid carcinoma (TT)-cell proliferation (potential therapeutic implication for cancer treatment); bilateral injection into the medulla reverses both tactile allodynia and thermal hyperalgesia.
 
L4545 L-798106 ≥98% (HPLC) L-798106 was among the first prostanoid receptor EP3-selective antagonists. It has been used in multiple studies to tease out EP3 agonist activity, both in vitro and in vivo. It successfully blocks the actions of sulprostone, an EP3-selective agonist, and it helped show that the vascular contraction effect of PGE2 is due to its prostanoid EP3 agonist activity.
 
A6730 Akt1/2 kinase inhibitor ≥98% (HPLC) Isozyme selective Akt1/2 kinase inhibitor. In in vitro kinase assays, Akt1/2 kinase inhibitor shows IC50 = 58 nM, 210 nM, and 2.12 mM for Akt1, Akt2, and Akt3, respectively, The inhibition appears to be pleckstrin homology (PH) domain-dependent and the Akt1/2 kinase inhibitor has no inhibitory effect against PH domain-lacking Akts, or other closely related AGC family kinases, PKA, PKC, and SGK, even at concentrations as high as 50 μM.
 
A7861 Asenapine maleate ≥98% (HPLC) Asenapine maleate is a 5-HT receptor antagonist (5-HT1A,1B, 5-HT2A, 2B, 2C, 5-HT5A, 5-HT6 and 5-HT7), a D2 antagonist, and an antipsychotic.
 
B8688 Biphenyl-indanone A ≥98% (HPLC), powder Biphenyl-indanone A (BINA) is a potent selective positive allosteric modulator for the group II metabotropic glutamate receptor subtype mGluR2. In animal studies BINA showed anxiolytic and antipsychotic effects, and blocked the effects produced by the hallucinogenic drug DOB. It decreased cocaine self-administration in rats, with no effect on food self-administration. In recombinant systems, BINA selectively potentiated the response of mGluR2 to glutamate with no effect on the glutamate response of other mGluR receptor subtypes tested.
 
C2247 CPPHA ≥98% (HPLC) CPPHA is a selective positive allosteric modulator of mGluR5 receptor. It has no agonist activity alone, but reduces threshold response and shifts dose-response curves to glutamate, quisqualate, and DHPG by 4- to 7-fold to the left in recombinant CHO cells expressing human or rat mGluR5.
 
C6022 Cyproheptadine hydrochloride sesquihydrate ≥98% (TLC), solid 5-HT2/5-HT1C serotonin receptor antagonist; H1 histamine receptor antagonist; antipruritic.
human ... HRH1(3269), HTR2A(3356), HTR2B(3357), HTR2C(3358)
D3821 Devazepide ≥98% (HPLC), powder Devazepide is a CCK1 (CCK-A) receptor antagonist and a CCK8 antagonist.
 
D1756 Dexamethasone ≥98% (HPLC), powder Glucocorticoid anti-inflammatory agent. Regulates T cell survival, growth, and differentiation. Inhibits the induction of nitric oxide synthase.
human ... ABCB1(5243), CYP3A4(1576), IL4(3565), IL5(3567), NR3C1(2908)
mouse ... Abcb1a(18671), Abcb1b(18669), Ifng(15978), Nos2(18126), Ptgs2(19225), Tnf(21926)
rat ... Ar(24208), Nr3c1(24413), Tnf(24835)
D8696 DMH4 >99.0% (HPLC) DMH4 is a potent VEGF inhibitor and an angiogenesis inhbitor. It is a selective VEGF inhibitor with an IC50 of 161 nM for VEGFR inhibition compared to 8000 nM for AMPK. Unlike the structurally similar DMH1, which is a selective BMP inhibitor, DMH4 shows little affinitiy for BMP with an IC50 of 3500 nM for BMPR-I.
 
D6446 DOV 216,303 ≥98% (HPLC) Triple reuptake inhibitor (TRI); serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI); IC50 values of ~20, 14, and 78 nM, respectively.
 
SML0197 4E1RCat ≥97% (HPLC) 4E1RCat ilnhibits the eIF4F translation initiation complex by binding to IF4E b and inhibiting the interaction between IF4E:eIF4G (IC50 = 3.2 μM). In in vitro translation experiments using MDA-MB-231 cells, 4E1RCat dose dependently inhibited cap-dependent translation, led to a decrease in polysome and 80S ribosomal subunits and reduced levels of the eIF4F-dependant proteins Mcl-1 and c-Myc.
 
E6888 Enalapril maleate salt powder, ≥98% (TLC) A long-acting angiotensin-converting enzyme inhibitor.
 
E9658 Enalaprilat dihydrate ≥98% (HPLC) Enalaprilat is an inhibitor of angiotensin converting enzyme (ACE), antihypertensive, and a Bradykinin B1 receptor activator. Enalaprilat has nM potency versus ACE and also activates B1 receptors to release NO.
 
A2734 α5IA ≥98% (HPLC) α5IA is a selective inverse agonist for Α5 subtype of GABAA receptor with a higher intrinsic activity at the A5 subtype than other drugs. α5IA enhances cognition in laboratory animals without being proconvulsant or anxiogenic. α5IA acts as an "alcohol antagonist," markedly reducing the amnesic effect of alcohol and partially attenuating sedation, similar to Ro15-4513, but without the anxiogenic effect. α5IA offers promise as a tool to study cognitive disorders, memory function, and treatment of alcohol-related disorders.
 
I0160 Imipenem monohydrate ≥98% (HPLC) Imipenem monohydrate is a broad spectrum B-lactam antibiotic. It is a member of the carbapenem class of "magic bullet" antibiotics for severe infections.
 
SML0189   Indinavir sulfate salt hydrate ≥98% (HPLC) Indinavir sulfate is an antiviral HIV protease inhibitor.
Indinavir sulfate suppresses the replication of HIV and is an important component of antiretroviral therapy for initial treatment of HIV infection. It is known to cause renal and urologic toxicity.
 
I8898 Ivermectin Positive allosteric modulator of α7 neuronal nicotinic acetylcholine receptor; also modulates glutamate-GABA-activated chloride channels.
human ... ABCB1(5243), CYP3A4(1576)
mouse ... Abcb1a(18671), Abcb1b(18669)
L1415 L-162,313 ≥95%, solid Non-peptide AT1 receptor agonist.
human ... AGTR1(185)
rat ... Agtr1(24180)
L2540 L-368,899 ≥98% (HPLC), powder L-368,899 is a non-peptide oxytocin receptor (OTR) antagonist.
human ... OXTR(5021)
L9787 L-655,708 ≥98% (HPLC), powder Novel ligand selective for the benzodiazepine site of GABAA receptors which contain the α5 subunit.
human ... GABRA5(2558)
L1790 L-685,458 >96% (HPLC), solid L-685,458 is a potent, selective, structurally novel γ-secretase inhibitor; equipotent inhibitor of both Aβ1-42 and Aβ1-40 production.
human ... APH1A(51107), APH1B(83464), NCSTN(23385), NOTCH1(4851), NOTCH2(4853), NOTCH3(4854), NOTCH4(4855), PSEN1(5663), PSEN2(5664), PSENEN(55851)
mouse ... Aph1a(226548), Aph1b(208117), Ncstn(59287), Notch1(18128), Notch2(18129), Notch3(18131), Notch4(18132), Psen1(19164), Psen2(19165), Psenen(66340)
rat ... Aph1a(365872), Aph1b(300802), Ncstn(289231), Notch1(25496), Notch2(29492), Notch3(56761), Notch4(406162), Psen1(29192), Psen2(81751), Psenen(292788)
L3040 L-765,314 hydrate ≥98% (HPLC), solid Potent and selective α1B-adrenoceptor antagonist.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146)
rat ... Adra1a(29412), Adra1b(24173), Adra1d(29413)
L9169 L-838,417 ≥98% (HPLC) L-838,417 is a novel pharmacology with no efficacy at a 1 subtype, but is partial agonist with equal efficacy at α2, K3 and α5 subtypes.
 
L6292 Lisinopril ≥98% (HPLC) Angiotensin converting enzyme (ACE) inhibitor.
human ... ACE(1636)
M4773 Metaraminol (+)-bitartrate salt α-adrenoceptor agonist.
 
M7571 MK-571 sodium salt hydrate ≥95% (HPLC) MK 571 is a potent and selective leukotriene D4 (LTD4) antagonist and ABCC multidrug resistance protein 1(MRP1) inhibitor. The cysteinyl leukotrienes (CysLTs), LTC4, LTD4, and LTE4, mediate their actions through two distinct G-protein coupled receptors. LTD4 is the preferred ligand for the CysLT1 receptor, whereas LTC4 and LTD4 bind with approximately equal affinity to the CysLT2 receptor. MK 571 is a selective, orally active CysLT1 receptor antagonist. It blocks the binding of LTD4, but not LTC4, to human and guinea pig lung membranes with Ki values of 0.22 nM and 2.1 nM, respectively. MK 571 effectively blocks LTD4 activation of recombinant human and mouse CysLT1 receptors but is ineffective at blocking LTC4 or LTD4 activation of the recombinant human or murine CysLT2 receptors. It potentially inhibits MRP1 and has been shown to overcome acquired arsenic tolerance.
 
M7065 MK-912 hydrochloride hydrate ≥98% (HPLC) Selective α2-adrenoceptor antagonist
human ... ADRB2(154)
M3074 MMPIP ≥98% (HPLC) MMPIP is a potent, selective, allosteric antagonist of metabotropic glutamate receptor 7 (mGluR7). It also displays intrinsic activity and acts as an inverse agonist.
 
SML0101 Montelukast sodium hydrate ≥98% (HPLC) Montelukast sodium hydrate is a leukotriene receptor antagonist (LTRA) used for the maintenance treatment of asthma and to relieve symptoms of seasonal allergies. It is a subtype specific CysLT1 receptor antagonist.
 
M4699 MTEP hydrochloride ≥98% (HPLC) MTEP is a potent and highly selective antagonist for mGluR5.
 
O1016 OPC-21268 hydrate ≥98% (HPLC) OPC-21268 is one of 2 non-peptide V1a selective antagonists, along with SR-49059. Arginine vasopressin (AVP) is a hormone that plays an important part in circulatory and water homoeostasis and is important in renal hemodynamic alterations, water retention, and cardiac remodeling in congestive heart failure (CHF). There are three AVP receptor subtypes-V1a, V1b, and V2 - all belong to the large rhodopsin-like G-protein-coupled receptor family. V(1a) antagonists improve water balance and cardiac hypertrophy in CHF and might be beneficial for the treatment of water retention and cardiac remodeling in CHF.
 
P8761 Probenecid    
S6196 Simvastatin ≥97% (HPLC), solid Simvastatin is a specific inhibitor of HMG-CoA reductase, the enzyme that catalyzes the conversion of HMG-CoA to mevalonate, an early step in cholesterol biosynthesis. It is used in the treatment of hypercholesterolemia, as it reduces levels of low-density lipoproteins and triglycerides, and raises high-density lipoprotein levels. Simvastatin is a lactone that is readily hydrolyzed in vivo to the corresponding β-hydroxyacid, and can be activated prior to use with NaOH in EtOH treatment. It is a synthetic analog of lovastatin (Cat. No. M2147).
Simvastatin, a synthetic analog of lovastatin, is a specific inhibitor of HMG-CoA reductase (3-hydroxy-3-methyl-glutaryl-CoA reductase.) HMG-CoA is a major therapeutic target for reduction of low density lipoprotein (LDL) cholesterol. Simvastatin may also have beneficial effects on endothelial function, smooth muscle cell function, hemostasis, vascular wall function, LDL oxidation, and inflammation. Simvastatin can be activated prior to use by treatment with NaOH in EtOH.
human ... HMGCR(3156)
rat ... Hmgcr(25675)
S8139 Sulindac ≥98.0% Nonsteroidal anti-inflammatory; preferential inhibitor of COX-1.
Sulindac is non-steroidal anti-inflammatory drug and an analgesic that has antiproliferative and apoptotic effects. It inhibits the expression and activity of cyclooxygenase-2 in human colon cancer cells25,26 and reduces tumor burden in adenomatous polyposis patients.27
human ... ALB(213), PTGS2(5743)
S1438   Sulindac sulfone ≥97% (TLC), (solid or powder) Metabolite of sulindac that inhibits cell growth by inducing apoptosis independently of cyclooxygenase inhibition. Inhibits the development and induces regression of premalignant adenomatous polyps.
Sulindac sulfone is non-steroidal anti-inflammatory drug and an analgesic that has antiproliferative and apoptotic effects. It inhibits the expression and activity of cyclooxygenase-2 in human colon cancer cells1,2 and reduces tumor burden in adenomatous polyposis patients.3
 
T6394 Timolol maleate salt ≥98% (TLC), powder Timolol maleate is a class II anti-arrhythmic agent that functions as a non-selective β-adrenoceptor antagonist, a vasodilator and an anti-glaucoma agent. Studies have reported that timolol maleate can be used for the treatment of infantile hemangioma (IH)7.
human ... ADRB1(153), ADRB2(154), ADRB3(155)
X2254 XE-991 ≥98% (HPLC) XE-991 is a KCNQ channel blocker; which is more potent than linopiridine (Cat. No. L-134).