Cas No.: | 307983-31-9 |
Chemical Name: | b-Alanine,N-[4-[[[trans-4-(1,1-dimethylethyl)cyclohexyl][[[4-(trifluoromethoxy)phenyl]amino]carbonyl]amino]methyl]benzoyl]- |
Synonyms: | b-Alanine,N-[4-[[[trans-4-(1,1-dimethylethyl)cyclohexyl][[[4-(trifluoromethoxy)phenyl]amino]carbonyl]amino]methyl]benzoyl]-;B-ALANINE, N-[4-[[[TRANS-4-(1,1-DIMETHYLETHYL)CYCLOHEXYL][[[4-(TRIFLUOROMETHOXY)PHENYL]AMINO]CARBONYL]AMINO]METHYL]BENZ...;GRA Ex-25;B-Alanine,N-[4-[[[trans-4-(1,1-dimethylethyl)cyclohexyl][[[4-(trifluoromethoxy)phenyl]amino]carbonyl]amino]methyl]benzoyl] |
SMILES: | O=C(O)CCNC(C1=CC=C(CN([C@H]2CC[C@H](C(C)(C)C)CC2)C(NC3=CC=C(OC(F)(F)F)C=C3)=O)C=C1)=O |
Formula: | C29H36N3O5F3 |
M.Wt: | 563.60844 |
Purity: | 98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | GRA Ex-25 is an inhibitor of glucagon receptor, with IC50 of 56 and 55 nM for rat and human glucagon receptors, 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[2]. |
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[1]. GRA Ex-25 has similar affinity to the rat and human glucagon receptors (IC50=56 and 55 nM, respectively)[2]. |