glucagon receptor antagonists-4 Chemical Properties

Boiling point:

675.0±55.0 °C(Predicted)

Density 

1.27±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMF: 50mg/mL; DMSO: 50mg/mL; DMSO:PBS (pH 7.2) (1:1): 0.5mg/mL; Ethanol: 0.5mg/mL

form 

A crystalline solid

pka

4.28±0.10(Predicted)

color 

White to off-white

InChIKey

IBDYYOQKQCCSDP-QFIPXVFZSA-N

SMILES

FC(F)(F)c1c[n](nc1)c2c(cc(cc2C)O[C@@H](CCC)c3ccc(cc3)C(=O)NCCC(=O)O)C

Safety Information

WGK Germany 

WGK 3

HS Code 

2933998090

Storage Class

11 - Combustible Solids

glucagon receptor antagonists-4 Usage And Synthesis

Uses

PF-06291874 is a novel and potent glucagon receptor antagonist for the potential treatment of diabetes mellitus. PF-06291874, has a lower molcular weight and lipophilicity than historical glucagon receptor antagonists, resulting in excellent selectivity in broad-panel screening, lower cytotoxicity, and excellent overall in vivo safety in early pre-clinical testing.

Biological Activity

PF-06291874 is an orally active, potent and selective glucagon receptor antagonist. PF-06291874 exhibits a robust glucose reductions in subjects with type 2 diabetes mellitus.

in vivo