1254730-81-8

1254730-81-8 structure

Name: SSTR5 antagonist 2
Chemical Name: 4-{8-[(2,6-diethoxy-4'-fluorobiphenyI-4-yl)methyl]-3-oxo-2,8-diazaspiro[4.5]dec-2-yl}benzoic acid
CAS Number: 1254730-81-8
Molecular Formula: C₃₂H₃₅FN₂O₅
Molecular Weight: 546.63
Catalog: Signaling Pathways GPCR/G Protein Somatostatin Receptor
Create Date: 2017-03-11 12:09:42
Modify Date: 2024-01-03 02:45:41
SSTR5 antagonist 2 (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].

Name	4-{8-[(2,6-diethoxy-4'-fluorobiphenyI-4-yl)methyl]-3-oxo-2,8-diazaspiro[4.5]dec-2-yl}benzoic acid

Description	SSTR5 antagonist 2 (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].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Somatostatin Receptor Research Areas >> Metabolic Disease
Target	SSTR5[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.