GW842166XCAS号： 666260-75-9分子式： C18H17Cl2F3N4O2分子量： 449.25描述纯度储存/保存方法外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)参考文献
| 产品描述 | |
| 描述 |
GW842166X is a selective non-cannabinoid CB2 receptor agonist, which is undergoing clinical development as a novel oral treatment for inflammatory pain |
| 纯度 |
>98%
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| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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| 基本信息 | |
| 外观 |
crystalline solid
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| 可溶性/溶解性 |
DMSO ：20 mg/mL (44.51 mM)
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| 生物活性 | |
| 靶点 |
CB2
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| In vitro(体外研究) |
GW842166X shows similar potency and efficacy for rat and human recombinant CB2 receptors with EC50 of 91 nM and 63nM, respectively. 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.
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| In vivo(体内研究) |
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. 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.
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| 参考文献 | |
| 参考文献 |
1. Giblin GM, et al. J Med Chem, 2007, 50(11), 2597-2600.2. Yao BB, et al. Br J Pharmacol, 2008, 153(2), 390-401.
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分子结构图
