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SSTR5 Antagonist 1 (compound 10) is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential for the research of treat type 2 diabetes mellitus (T2DM)[1]. | [in vivo]
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. |
| [References]
[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. DOI:10.1021/acsmedchemlett.8b00305 |
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