GRA Ex-25

Preparation Method

The receptor and small ligand molecules Gra EX-25 were used to conduct molecular docking of 5XEZ-A with dauricine and Gra Ex-25 using Vina computing under the calculation conditions screened. In addition, scoring data and PyMol were used to analyze the ligand and receptor amino acid binding way.

Applications

Gra Ex-25 is bonded to Ser350 and Lys349 amino acids of GCGR through hydrogen bonding.

Animal models

Glucagon challenged rats

Preparation Method

Anesthetized animals were given an intravenous dose of GRA Ex-25 min prior to a 3 ¦̧/kg glucagon load.

Dosage form

1-3mg/ml GRA Ex-25

Applications

GRA Ex-25 (3 mg/kg) significantly reduced blood glucose levels in rats with elevated blood glucose induced by exogenous glucagon.

References:

[1]. Li L, Dai S, et,al . Antagonistic Effect and In Vitro Activity of Dauricine on Glucagon Receptor. J Nat Prod. 2022 Aug 26;85(8):2035-2043. doi: 10.1021/acs.jnatprod.2c00446. Epub 2022 Jul 14. PMID: 35834753.
[2].Lau J, Behrens C, et,al . New beta-alanine derivatives are orally available glucagon receptor antagonists. J Med Chem. 2007 Jan 11;50(1):113-28. doi: 10.1021/jm058026u. PMID: 17201415.