Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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 | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 30.00 | |
2 mg | In stock | $ 43.00 | |
5 mg | In stock | $ 70.00 | |
10 mg | In stock | $ 125.00 | |
25 mg | In stock | $ 235.00 | |
50 mg | In stock | $ 348.00 | |
100 mg | In stock | $ 518.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 68.00 |
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 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 |
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)
You can also refer to dose conversion for different animals. More
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
GW842166X 666260-75-9 GPCR/G Protein Cannabinoid Receptor inhibit GW-842166X Inhibitor inhibitor