Adomeglivant_product_DataBase

Bioactivity

Adomeglivant (LY2409021) is a potent, selective glucagon receptor (GluR) allosteric antagonist. Adomeglivant is widely used in the research for type 2 diabetes mellitus[1][2][3].

Target

GluR

Invitro

Adomeglivant dose-dependently blocks glucagon-induced the raise levels of cAMP in HEK293-GluR cells[2].Adomeglivant fails to block cAMP-elevating actions of adenosine[2].Adomeglivant exhibits high selectivity for family B GPCRs, and specifically interacts with a conserved binding motif within the GluR, GLP-1R, and GIP-R[2].

In Vivo

Adomeglivant (5 mg/kg; i.p.) completely abolishes the hyperglycaemic action of CNO (clozapine-N-oxide) in Avpires-Cre+ 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.)[3] Animal Model:

Name

Adomeglivant

CAS

1488363-78-5

Formula

C32H36F3NO4

Molar Mass

555.63

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Sonam Grover, et al. Computational identification of novel natural inhibitors of glucagon receptor for checking type II diabetes mellitus. BMC Bioinformatics. 2014; 15(Suppl 16): S13. [2]. Oleg G Chepurny, et al. Non-conventional glucagon and GLP-1 receptor agonist and antagonist interplay at the GLP-1 receptor revealed in high-throughput FRET assays for cAMP. J Biol Chem. 2019 Mar 8;294(10):3514-3531. [3]. Angela Kim, et al. AVP-induced counter-regulatory glucagon is diminished in type 1 diabetes. bioRxiv. January 31, 2020.

PeptideDB

Adomeglivant

CAS: 1488363-78-5 F: C32H36F3NO4 W: 555.63