An agonist of GPR119 (EC50s = 46 and 421 nM for the human and rat receptors

APD597 – 50 mg

Brand:
Cayman
CAS:
897732-93-3
Storage:
-20
UN-No:
Non-Hazardous - /

APD597 is an orally bioavailable agonist of GPR119 that has EC50 values of 46 and 421 nM for the human and rat receptors, respectively, in a homologous time-resolved fluorescence (HTRF) assay.{48588} It increases insulin secretion stimulated by a high, but not low, concentration of glucose in isolated mouse pancreatic β-cells and in isolated human islets.{48589} APD597 (20 mg/kg) increases levels of glucagon-like peptide-1 (GLP-1; Item No. 24460) induced by glucose in mice. It also decreases blood glucose levels in an oral glucose tolerance test in mice when administered at doses of 1 and 10 mg/kg and in Zucker diabetic rats at a dose of 3 mg/kg.{48588}  

 

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Description

An agonist of GPR119 (EC50s = 46 and 421 nM for the human and rat receptors, respectively, in an HTRF assay); increases high glucose-induced insulin secretion in isolated mouse pancreatic β-cells and isolated human islets; increases glucose-induced GLP-1 levels in mice at 20 mg/kg; decreases blood glucose levels in an oral glucose tolerance test in mice at 1 and 10 mg/kg and in Zucker diabetic rats at 3 mg/kg

Formal name: 4-[[5-methoxy-6-[[2-methyl-6-(methylsulfonyl)-3-pyridinyl]amino]-4-pyrimidinyl]oxy]-1-piperidinecarboxylic acid, 1-methylethyl ester

Synonyms:  JNJ-38431055

Molecular weight: 479.6

CAS: 897732-93-3

Purity: ≥98%

Formulation: A crystalline solid

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

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