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GPR39-C3 is a potent agonist of the orphan G protein-coupled receptor GPR39, selectively targeting GPR39 over a range of other receptors and enzymes. It demonstrates high efficacy in promoting cAMP production in both human and rat receptors, with low EC50 values. GPR39-C3 also enhances the secretion of glucagon-like peptide 1 (GLP-1) and provides protection against cytokine-induced cell death in specific cell lines. In vivo, it significantly increases the amount of active GLP-1 in glucose-challenged mice when co-administered with a DPP-4 inhibitor.

1621175-65-2

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1621175-65-2 Usage

Uses

Used in Pharmaceutical Industry:
GPR39-C3 is used as a potent agonist for the orphan G protein-coupled receptor GPR39, specifically targeting this receptor over a panel of kinases, ghrelin, neurotensin-1 receptors, and various enzymes, transporters, or G protein-coupled receptors. Its high selectivity and potency make it a valuable compound for the development of new therapeutic strategies.
Used in Diabetes Research and Treatment:
GPR39-C3 is used as a therapeutic agent for diabetes, particularly in increasing the secretion of glucagon-like peptide 1 (GLP-1) in STC-1 mouse enteroendocrine cells. This action can help improve glucose homeostasis and provide a potential treatment option for diabetes management.
Used in Cell Protection:
GPR39-C3 is used as a protective agent against cytokine-induced cell death in INS-1E rat insulinoma cells, showcasing its potential in safeguarding cells from harmful cytokine effects, which could be beneficial in various cell-based therapies and treatments.
Used in In Vivo Studies:
GPR39-C3 is used in in vivo studies to investigate its effects on glucose-challenged mice when administered with a DPP-4 inhibitor. The compound has demonstrated a significant increase in the amount of active GLP-1 in sera, indicating its potential use in enhancing GLP-1 activity and glucose regulation in vivo.

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.

1621175-65-2Downstream Products

1621175-65-2Relevant academic research and scientific papers

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

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