Target Validation Information
TTD ID	T93788
Target Name	Glucose-dependent insulinotropic receptor (GPR119)
Type of Target	Successful
Drug Potency against Target	APD668	Drug Info	EC50 = 2.51 nM	[2]
Action against Disease Model	APD668	Drug Info	APD668 increases adenylate cyclase activation in HEK293 cells transfected with h uMan GPR119 (but not in non-transfected cells) in a concentration-dependent manner with an EC50 of 23 nM. It also enhanced insulin release from both rat and h uMan isolated pancreatic islets in a glucose-dependent manner. in Zucker Diabetic Fatty (ZDF) rats. APD668 significantly reduced blood glucose and glycated hemoglobin (HbA1c) levels over eight weeks of treatment (QD), with no desensitization of the acute drug response over this period at 30 mg/kg po	[1]
References
REF 1	Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control. Bioorg Med Chem Lett. 2011 May 15;21(10):3134-41.
REF 2	GPR119 agonists: a promising new approach for the treatment of type 2 diabetes and related metabolic disorders. Curr Opin Drug Discov Devel. 2009 Jul;12(4):519-32.

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