GRA Ex-25( GRA Ex-25 | GRA Ex 25 | GRA Ex25 | GRAEx-25 )

Catalog No. M13984 CAS No. 307983-31-9

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Datasheet

HNMR

HPLC

MSDS

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Product Name

GRA Ex-25
Note

Research use only, not for human use.
Brief Description

A potent glucagon receptor inhibitor with IC50 of 56 and 55 nM for rat and human glucagon receptors.
Description

A potent glucagon receptor inhibitor with IC50 of 56 and 55 nM for rat and human glucagon receptors; binds to human glucagon receptor with Ki of 63 nM, moderately inhibits glucagon induced adenylate cyclase (Ki=254 nM); significantly reduces blood glucose caused by exogenous administration of glucagon in rat model (3 mg/kg, i.v.).Diabetes Preclinical.
In Vitro

GRA Ex-25 binds a human glucagon receptor (h-GlucRbind) with Ki of 63 nM and a moderate glucagon induced adenylate cyclase inhibition (h-GlucRcyclase) with Ki of 254 nM under our assay conditions. GRA Ex-25 has similar affinity to the rat and human glucagon receptors (IC50=56 and 55 nM, respectively).
In Vivo

GRA Ex-25 (3 mg/kg, i.v.) significantly reduces blood glucose caused by exogenous administration of glucagon in rat model. GRA Ex-25 is able to inhibit the rise in blood glucose levels elicited by exogenous administered glucagon, most likely because of the direct inhibition of glucagon stimulated hepatic glucose output.
Synonyms

GRA Ex-25 | GRA Ex 25 | GRA Ex25 | GRAEx-25
Pathway

GPCR/G Protein
Target

Glucagon Receptor
Recptor

humanglucagonreceptor|ratglucagonreceptor
Research Area

Metabolic Disease
Indication

Diabetes

CAS Number

307983-31-9
Formula Weight

563.6085
Molecular Formula

C29H36F3N3O5
Purity

>98% (HPLC)
Solubility

DMSO: ≥ 32 mg/mL
SMILES

C[C@](C1CC[C@H](N(C(NC2C=CC(OC(F)(F)F)=CC=2)=O)CC2C=CC(C(NCCC(O)=O)=O)=CC=2)CC1)(C)C
Chemical Name

β-Alanine, N-[4-[[[trans-4-(1,1-dimethylethyl)cyclohexyl][[[4-(trifluoromethoxy)phenyl]amino]carbonyl]amino]methyl]benzoyl]-

1. Kurukulasuriya R, et al. Bioorg Med Chem Lett. 2004 May 3;14(9):2047-50. 2. Lau J, et al. J Med Chem. 2007 Jan 11;50(1):113-28.

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