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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $30 | In Stock | |
2 mg | $43 | In Stock | |
5 mg | $70 | In Stock | |
10 mg | $125 | In Stock | |
25 mg | $235 | In Stock | |
50 mg | $348 | In Stock | |
100 mg | $518 | In Stock | |
1 mL x 10 mM (in DMSO) | $68 | In Stock |
Description | 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. |
In vitro | 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] |
In vivo | 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] |
Molecular Weight | 449.25 |
Formula | C18H17Cl2F3N4O2 |
Cas No. | 666260-75-9 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | |||||||||||||||
Solubility Information | Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 16 mg/mL (35.6 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||
Solution Preparation Table | ||||||||||||||||
DMSO
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