A potent agonist of GPR119 (EC50s = 2.7 and 33 nM for human and rat forms

APD668 – 5 mg

Brand:
Cayman
CAS:
832714-46-2
Storage:
-20
UN-No:
Non-Hazardous - /

GPR119, a glucose-dependent insulinotropic receptor, is a G protein-coupled receptor that is expressed in pancreatic β-cells and intestinal L-cells.{14046} Activation of GPR119 by the endogenous ligands lyso-phosphatidylcholine (Item No. 10172) and oleoyl ethanolamide (Item No. 90265) increases intracellular cAMP levels and promotes glucose-stimulated insulin secretion.{14046,18880} APD668 is a potent agonist of GPR119 (EC50s = 2.7 and 33 nM for human and rat forms, respectively).{28680} Chronic dosing with APD668 in Zucker diabetic fatty rats over several weeks significantly reduces blood glucose and glycated hemoglobin levels.{28680}  

 

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Description

A potent agonist of GPR119 (EC50s = 2.7 and 33 nM for human and rat forms, respectively); significantly reduces blood glucose and glycated hemoglobin levels in Zucker diabetic fatty rats

Formal name: 4-[[1-[2-fluoro-4-(methylsulfonyl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-4-yl]oxy]-1-piperidinecarboxylic acid, 1-methylethyl ester

Synonyms:  JNJ-28630368

Molecular weight: 477.5

CAS: 832714-46-2

Purity: ≥95%

Formulation: A crystalline solid

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

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