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

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