Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GW842166X 是一种选择性 cannabinoid receptor 2 激活剂,IC50=63 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 289 | 现货 | ||
2 mg | ¥ 413 | 现货 | ||
5 mg | ¥ 728 | 现货 | ||
10 mg | ¥ 1,120 | 现货 | ||
25 mg | ¥ 1,830 | 现货 | ||
50 mg | ¥ 2,720 | 现货 | ||
100 mg | ¥ 3,980 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 722 | 现货 |
产品描述 | 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. |
靶点活性 | CB2:63 nM(EC50) |
体外活性 | 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] |
体内活性 | 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] |
别名 | 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 |
分子量 | 449.25 |
分子式 | C18H17Cl2F3N4O2 |
CAS No. | 666260-75-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 16 mg/mL (35.6 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2259 mL | 11.1297 mL | 22.2593 mL | 55.6483 mL |
5 mM | 0.4452 mL | 2.2259 mL | 4.4519 mL | 11.1297 mL | |
10 mM | 0.2226 mL | 1.113 mL | 2.2259 mL | 5.5648 mL | |
20 mM | 0.1113 mL | 0.5565 mL | 1.113 mL | 2.7824 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
GW842166X 666260-75-9 GPCR/G Protein Cannabinoid Receptor inhibit 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 GW-842166X Inhibitor inhibitor