| Chemical Properties | Back Directory | [Boiling point ]
622.8±55.0 °C(Predicted) | [density ]
1.393±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 5 mg/ml; DMSO: 3 mg/ml; Ethanol: 10 mg/ml; Ethanol:PBS (pH 7.2) (1:3): 0.25 mg/ml | [pka]
1.09±0.50(Predicted) |
| Hazard Information | Back Directory | [Uses]
GW 848687X is a selective, orally active prostaglandin EP1 receptor antagonist for the inhibition of inflammatory pain. The oral bioavailability of GW 848687X was 54% in rats and 53% in dogs. GW 848687X has a half-life of 2 hours and has inhibitory potential for both acute and chronic pain[1]. | [in vivo]
GW 848687X (30 mg/kg; po; b.i.d, 5 d) exhibits antihyperalgesic activity in an FCA-induced inflammatory joint pain model[1].
| Animal Model: | FCA induced joint pain model of inflammatory pain[1] | | Dosage: | 30mg/kg | | Administration: | po; twice daily for 5 days | | Result: | Completely reversed pain sensation in rats and had anti-pain effects. |
| [References]
[1] Giblin GM, et al. The discovery of 6-[2-(5-chloro-2-{[(2,4-difluorophenyl)methyl]oxy}phenyl)-1-cyclopenten-1-yl]-2-pyridinecarboxylic acid, GW848687X, a potent and selective prostaglandin EP1 receptor antagonist for the treatment of inflammatory pain. Bioorg Med Chem Lett. 2007 Jan 15;17(2):385-9. DOI:10.1016/j.bmcl.2006.10.041 |
|
|