A potent GPR39 agonist (EC50s = 0.8 and 0.4 nM for cAMP production in HEK293 cells expressing human and rat receptors

GPR39-C3 – 1 mg

Brand:
Cayman
CAS:
1621175-65-2
Storage:
-20
UN-No:
Non-Hazardous - /

GPR39-C3 is a potent agonist of the orphan G protein-coupled receptor GPR39 with EC50 values of 0.8 and 0.4 nM for cAMP production in HEK293 cells expressing human and rat receptors, respectively.{42282} It is selective for GPR39 over a panel of kinases (IC50s = >10 μM), ghrelin and neurotensin-1 receptors (IC50s = >30 μM), and a variety of enzymes, transporters, or G protein-coupled receptors. GPR39-C3 increases secretion of glucagon-like peptide 1 (GLP-1; Item No. 24460) in STC-1 mouse enteroendocrine cells (EC50 = 0.06 μM) and is protective against cytokine-induced cell death in INS-1E rat insulinoma cells (EC50 = 0.02 μM). In vivo, GPR39-C3 (30 mg/kg) increases the amount of active GLP-1 in sera by 6-fold in glucose-challenged mice when administered concurrently with a dipeptidyl peptidase 4 (DPP-4) inhibitor.  

 

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Description

A potent GPR39 agonist (EC50s = 0.8 and 0.4 nM for cAMP production in HEK293 cells expressing human and rat receptors, respectively); selective for GPR39 over a panel of kinases (IC50s = >10 μM), ghrelin and neurotensin-1 receptors (IC50s = >30 μM), and a variety of enzymes, transporters, or G protein-coupled receptors; increases secretion of GLP-1 in STC-1 cells (EC50 = 0.06 μM); is protective against cytokine-induced cell death in INS-1E cells (EC50 = 0.02 μM); increases the amount of active GLP-1 in sera in glucose-challenged mice when administered concurrently with a DPP-4 inhibitor at 30 mg/kg,

Formal name: N-[3-chloro-4-[[[2-(methylamino)-6-(2-pyridinyl)-4-pyrimidinyl]amino]methyl]phenyl]-methanesulfonamide

Synonyms: 

Molecular weight: 418.9

CAS: 1621175-65-2

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes

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