SSTR5 antagonist 2 TFA

SSTR5 Antagonist 1 (compound 10) is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential to treat type 2 diabetes mellitus (T2DM)[1].

Signaling Pathways >> GPCR/G Protein >> Somatostatin Receptor

Research Areas >> Metabolic Disease

SSTR5[1].

SSTR5 antagonist 2 (10 mg/kg, orally) increases both total and active circulating incretin hormone GLP1 levels in mice at a dose of 10 mg/kg[1]. SSTR5 antagonist 2 increases pancreatic insulin secretion as well as total and active GLP1 release, and demonstrates synergistic effects in combination with DPP4 inhibitors[1]. Animal Model: Rodent diabetic model without risk of hypoglycemia[1]. Dosage: 10 mg/kg. Administration: Orally. Result: Increased both total and active circulating incretin hormone GLP1 levels.

[1]. Liu W, et al. Discovery and Pharmacology of a Novel Somatostatin Subtype 5 (SSTR5) Antagonist: Synergy with DPP-4 Inhibition. ACS Med Chem Lett. 2018 Sep 12;9(11):1082-1087.