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BOC Sciences |
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| | GRA Ex-25 Basic information |
| Product Name: | GRA Ex-25 | | Synonyms: | GRA Ex-25;B-Alanine, N-[4-[[[trans-4-(1,1-dimethylethyl)cyclohexyl][[[4-(trifluoromethoxy)phenyl]amino]carbonyl]amino]methyl]benzoyl]-;β-Alanine, N-[4-[[[trans-4-(1,1-dimethylethyl)cyclohexyl][[[4-(trifluoromethoxy)phenyl]amino]carbonyl]amino]methyl]benzoyl]-;GRA Ex-25 USP/EP/BP;GRA Ex-25[GRA-Ex-25;GCGR,inhibit,GRA Ex 25,Inhibitor,GRA Ex-25,Glucagon Receptor,GRA Ex25;3-(4-((1-(trans-4-(tert-Butyl)cyclohexyl)-3-(4-(trifluoromethoxy)phenyl)ureido)methyl)benzamido)propanoic acid;3-{[4-({1-[(1r,4r)-4-tert-butylcyclohexyl]{[4-(trifluoromethoxy)phenyl]carbamoyl}amino}methyl)phenyl]formamido}propanoic acid | | CAS: | 307983-31-9 | | MF: | C29H36F3N3O5 | | MW: | 563.61 | | EINECS: | | | Product Categories: | | | Mol File: | 307983-31-9.mol |  |
| | GRA Ex-25 Chemical Properties |
| 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| |
| | GRA Ex-25 Usage And Synthesis |
| 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]. | | 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 |
| | GRA Ex-25 Preparation Products And Raw materials |
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