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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.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $42 | In Stock | In Stock | |
| 10 mg | $75 | In Stock | In Stock | |
| 25 mg | $141 | In Stock | In Stock | |
| 50 mg | $208 | In Stock | In Stock | |
| 100 mg | $292 | In Stock | In Stock | |
| 200 mg | $417 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $41 | In Stock | 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. |
| Targets&IC50 | CB2:63 nM(EC50) |
| In vitro | GW842166X demonstrates comparable potency and efficacy for rat and human recombinant CB2 receptors, with EC50 values of 91 nM and 63 nM, respectively. [1] It exhibits full agonist activity in cyclase assays with an EC50 of 133 nM and an Emax of 101%, and weak agonist activity in FLIPR assays with an EC50 of 7.780 μM and an Emax of 84%. [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 |
| Smiles | FC(F)(F)c1nc(Nc2cc(Cl)cc(Cl)c2)ncc1C(=O)NCC1CCOCC1 |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 16 mg/mL (35.61 mM), Sonication is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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