GW842166X 是一种选择性 Cannabinoid Receptor 2 激活剂，IC50=63 nM。

GW842166X is a potent and highly selective agonist of cannabinoid receptor CB2 receptor with EC50 of 63 nM, shows no significant activity at CB1 receptor. Phase 2.

GW842166X shows similar potency and efficacy for rat and human recombinant CB2 receptors with EC50 of 91 nM and 63 nM, respectively. [1] GW-842166X exhibits full agonist potency with an EC50 of 133 nM and Emax of 101% in cyclase assays. GW-842166X exhibits weak agonist potency with an EC50 of 7.780 μM and Emax of 84% in FLIPR assays. [2]

GW842166X has an oral bioavailability of 58% and a half-life of 3 h when dosed orally in the rat. GW842166X has extremely high potency with an oral ED50 of 0.1 mg/kg and shows full reversal of hyperalgesia at 0.3 mg/kg in the FCAa model of inflammatory pain. [1] GW842166X orally administrated at a dose of 15 mg/kg for 8 days produced a significant reversal of the CCI induced decrease in paw withdrawal threshold in a rat model of neuropathic pain. [3]

666260-75-9

C18H17Cl2F3N4O2

449.26

2-(2,4-二氯苯基氨基)-4-三氟甲基嘧啶-5-羧酸[(四氢吡喃-4-基)甲基]酰胺

DMSO:16 mg/mL (35.6 mM)
H2O:<1 mgml
Ethanol:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years