Molecular Formula | C18H17Cl2F3N4O2 |
Molar Mass | 449.25 |
Storage Condition | -20℃ |
In vitro study | GW842166X had similar potency at the rat and human recombinant protein CB2 receptors, with EC 50 of 91 nM and 63nM, respectively. The EC 50 value for full Agonist Efficacy GW-842166X was 133 and the E max was 101% on the cyclase assay. Its EC 50 for the detection of incomplete agonist potency by FLIPR was 7.780nm and the E max was 84%. |
In vivo study | The oral bioavailability of GW842166X in the rat model was 58%, and the Half-Life was 3 hours. Its high efficacy, oral ED 50 0.1mg/kg. The 0.3mg/kg dose reverses pain sensation in the FCAa model of inflammatory pain. GW842166X at an oral dose of 15mg/kg for 8 days significantly reduced the foot threshold in a CCI-induced neuropathic pain rat model. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.226 ml | 11.13 ml | 22.259 ml |
5 mM | 0.445 ml | 2.226 ml | 4.452 ml |
10 mM | 0.223 ml | 1.113 ml | 2.226 ml |
5 mM | 0.045 ml | 0.223 ml | 0.445 ml |