| Identification | Back Directory | [Name]
GRA Ex-25 | [CAS]
307983-31-9 | [Synonyms]
GRA Ex-25
GRA Ex-25 USP/EP/BP
β-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]benzoyl]- | [Molecular Formula]
C29H36F3N3O5 | [MDL Number]
MFCD11977277 | [MOL File]
307983-31-9.mol | [Molecular Weight]
563.61 |
| Chemical Properties | Back Directory | [Melting point ]
152-154 °C | [Boiling point ]
726.3±60.0 °C(Predicted) | [density ]
1.28±0.1 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,Store in freezer, under -20°C | [solubility ]
DMF:25.0(Max Conc. mg/mL);44.36(Max Conc. mM)
DMSO:28.5(Max Conc. mg/mL);50.57(Max Conc. mM)
DMF:PBS (pH 7.2) (1:8):0.1(Max Conc. mg/mL);0.18(Max Conc. mM)
Ethanol:10.0(Max Conc. mg/mL);17.74(Max Conc. mM) | [form ]
A crystalline solid | [pka]
4.29±0.10(Predicted) | [color ]
White to off-white | [InChIKey]
BZXMLCVDKDXRQY-AFARHQOCNA-N | [SMILES]
C(C)(C)([C@@H]1CC[C@H](CC1)N(CC1=CC=C(C=C1)C(=O)NCCC(=O)O)C(=O)NC1=CC=C(C=C1)OC(F)(F)F)C |&1:3,6,r| |
| Hazard Information | Back Directory | [Uses]
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]. | [storage]
Store at -20°C | [References]
[1] Kurukulasuriya R, et al. Biaryl amide glucagon receptor antagonists. Bioorg Med Chem Lett. 2004 May 3;14(9):2047-50. DOI:10.1016/j.bmcl.2004.02.056
[2] Kurukulasuriya R, et al. Biaryl amide glucagon receptor antagonists. Bioorg Med Chem Lett. 2004 May 3;14(9):2047-50. DOI:10.1021/jm058026u |
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