| Identification | Back Directory | [Name]
glucagon receptor antagonists-4 | [CAS]
1393124-08-7 | [Synonyms]
CS-2641
PF6291874
GCGR-IN-17
PF-06291874 >=98% (HPLC)
lucagon receptor antagonists-4
Glucagon Receptor Antagonist 4
glucagon receptor antagonists-4
PF06291874;PF-06291874;PF 06291874
PF-06291874(glucagon receptor antagonists-4)
N-{4-[(1S)-1-{3,5-Dimethyl-4-[4-(trifluoromethyl)-1H-pyrazol-1-yl]phenoxy}butyl]benzoyl}-β-alanine
β-Alanine, N-[4-[(1S)-1-[3,5-dimethyl-4-[4-(trifluoromethyl)-1H-pyrazol-1-yl]phenoxy]butyl]benzoyl]- | [Molecular Formula]
C26H28F3N3O4 | [MDL Number]
MFCD30343861 | [MOL File]
1393124-08-7.mol | [Molecular Weight]
503.51 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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 activepotent and selective glucagon receptor antagonist. PF-06291874 exhibits a robust glucose reductions in subjects with type 2 diabetes mellitus. | [in vivo]
PF-06291874 exposure is approximately dose-proportional with a half-life of ～19.7-22.7 h. PF-06291874 has a fast on and off rate. PF-06291874 is highly bound to human plasma protein, with a mean free fraction of ～0.55%[3]. | [storage]
Store at -20°C |
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