1621175-65-2 Usage
Description
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. 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; ) 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.
Uses
TC-G 1008 is the first potent, selective, and orally bioavailable GPR39 agonist.
Check Digit Verification of cas no
The CAS Registry Mumber 1621175-65-2 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,6,2,1,1,7 and 5 respectively; the second part has 2 digits, 6 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 1621175-65:
(9*1)+(8*6)+(7*2)+(6*1)+(5*1)+(4*7)+(3*5)+(2*6)+(1*5)=142
142 % 10 = 2
So 1621175-65-2 is a valid CAS Registry Number.
1621175-65-2Relevant articles and documents
Discovery of 2-pyridylpyrimidines as the first orally bioavailable GPR39 agonists
Peukert, Stefan,Hughes, Richard,Nunez, Jill,He, Guo,Yan, Zhao,Jain, Rishi,Llamas, Luis,Luchansky, Sarah,Carlson, Adam,Liang, Guiqing,Kunjathoor, Vidya,Pietropaolo, Mike,Shapiro, Jeffrey,Castellana, Anja,Wu, Xiaoping,Bose, Avirup
, p. 1114 - 1118 (2014)
The identification of highly potent and orally bioavailable GPR39 agonists is reported. Compound 1, found in a phenotypic screening campaign, was transformed into compound 2 with good activity on both the rat and human GPR39 receptor. This compound was fu
