An allosteric antagonist of the glucagon receptor; inhibits glucagon-induced increases in cAMP levels in HEK293 cells expressing the rat glucagon or GLP-1 receptors (IC50s = 1.8 and 1.2 µM

Adomeglivant – 1 mg

Brand:
Cayman
CAS:
1488363-78-5
Storage:
-20
UN-No:
Non-Hazardous - /

Adomeglivant is an allosteric antagonist of the glucagon receptor.{47796,47797} It inhibits glucagon-induced increases in cAMP levels in HEK293 cells expressing the rat glucagon or GLP-1 receptors (IC50s = 1.8 and 1.2 µM, respectively) but has no effect on cAMP levels when used alone.{47797} Adomeglivant also inhibits increases in cAMP levels induced by GLP-1 or exendin-4 (Item No. 11096) in HEK293 cells expressing the GLP-1 receptor (IC50s = 7 and 12 µM, respectively). It decreases glucose-stimulated insulin secretion when used at a concentration of 1 µM in combination with the GLP-1 receptor antagonist exendin (9-39) in isolated human islets but not glucose-stimulated glucagon secretion when used alone or in combination with exendin (9-39) in isolated mouse islets.{47798}  

 

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SKU: 29668 - 1 mg Category:

Description

An allosteric antagonist of the glucagon receptor; inhibits glucagon-induced increases in cAMP levels in HEK293 cells expressing the rat glucagon or GLP-1 receptors (IC50s = 1.8 and 1.2 µM, respectively) but has no effect on cAMP levels when used alone; inhibits increases in cAMP levels induced by GLP-1 or exendin-4 in HEK293 cells expressing the GLP-1 receptor (IC50s = 7 and 12 µM, respectively); decreases glucose-stimulated insulin secretion at 1 µM in combination with exendin (9-39) in isolated human islets but not glucose-stimulated glucagon secretion alone or in combination with exendin (9-39) in isolated mouse islets

Formal name: N-[4-[(1S)-1-[[4′-(1,1-dimethylethyl)-2,6-dimethyl[1,1′-biphenyl]-4-yl]oxy]-4,4,4-trifluorobutyl]benzoyl]-β-alanine

Synonyms:  LY2409021

Molecular weight: 555.6

CAS: 1488363-78-5

Purity: ≥98%

Formulation: A solid

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