ChemicalBook--->CAS DataBase List--->1254730-81-8

1254730-81-8

1254730-81-8 Structure

1254730-81-8 Structure
IdentificationBack Directory
[Name]

MK-5582
[CAS]

1254730-81-8
[Synonyms]

MK-5582
SSTR5 antagonist 2
SSTR5 antagonist 2,SSTR-5 antagonist 2
4-{8-[(2,6-diethoxy-4'-fluorobiphenyI-4-yl)Methyl]-3-oxo-2,8-diazaspiro[4.5]dec-2-yl}benzoic acid
Benzoic acid, 4-[8-[(2,6-diethoxy-4'-fluoro[1,1'-biphenyl]-4-yl)methyl]-3-oxo-2,8-diazaspiro[4.5]dec-2-yl]-
4-(8-((2,6-diethoxy-4'-fluoro-[1,1'-biphenyl]-4-yl)Methyl)-3-oxo-2,8-diazaspiro[4.5]decan-2-yl)benzoic acid
[Molecular Formula]

C32H35FN2O5
[MDL Number]

MFCD18633148
[MOL File]

1254730-81-8.mol
[Molecular Weight]

546.63
Chemical PropertiesBack Directory
[Boiling point ]

710.2±60.0 °C(Predicted)
[density ]

1.30±0.1 g/cm3(Predicted)
[pka]

4.34±0.10(Predicted)
Hazard InformationBack Directory
[Uses]

SSTR5 antagonist 2 (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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