GRA Ex-25 |
| カタログ番号GC31379 |
GRA Ex-25 はグルカゴン受容体の阻害剤であり、IC50 はラットおよびヒトのグルカゴン受容体に対してそれぞれ 56 および 55 nM です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 307983-31-9
Sample solution is provided at 25 µL, 10mM.
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GRA Ex-25 is a potent glucagon receptor inhibitor with IC50 of 56 and 55 nM for rat and human glucagon receptors, respectively. GRA Ex-25 binds to the human glucagon receptor (h-GlucRbind) with a Ki of 63 nM and moderates glucagon-induced adenylate cyclase inhibition (h-GlucRcyclase) with a Ki of 254 nM[2]. GRA Ex-25 has similar affinity for rat and human glucagon receptors (IC50 of 56 and 55 nM, respectively). GRA Ex-25 (3 mg/kg, iv) reduces blood glucose levels induced by exogenous glucagon in a rat model, possibly due to direct inhibition of glucagon-stimulated hepatic glucose output[2].
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.
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