Adomeglivant (LY2409021) is a potent, selective glucagon receptor (GluR) allosteric antagonist. Adomeglivant is widely used in the research for type 2 diabetes mellitus.
IC50&Target
GluR
体外研究
Adomeglivant dose-dependently blocks glucagon-induced the raise levels of cAMP in HEK293-GluR cells.
Adomeglivant fails to block cAMP-elevating actions of adenosine.
Adomeglivant exhibits high selectivity for family B GPCRs, and specifically interacts with a conserved binding motif within the GluR, GLP-1R, and GIP-R.
体内研究
Adomeglivant (5 mg/kg; i.p.) completely abolishes the hyperglycaemic action of CNO (clozapine-N-oxide) in Avp mice. (CNO is a specific, pharmacologically inert agonist for hM3Dq-induced membrane depolarisation and increased the firing rate in hM3Dq-expressing arginine-vasopressin (AVP) neurons.)
Animal Model:
Avp mice
Dosage:
5 mg/kg
Administration:
Intraperitoneal injection, 30 minutes prior to CNO
Result:
Completely abolished the hyperglycaemic action of CNO.
分子式
C32H36F3NO4
分子量
555.63
CAS号
1488363-78-5
中文名称
阿度格列凡
运输条件
Room temperature in continental US; may vary elsewhere.