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GW842166X

Catalog No. T6527Cas No. 666260-75-9

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.

GW842166X

GW842166X

Purity: 99.47%
Catalog No. T6527Cas No. 666260-75-9
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 SizePriceAvailabilityQuantity
1 mg$30In Stock
2 mg$43In Stock
5 mg$70In Stock
10 mg$125In Stock
25 mg$235In Stock
50 mg$348In Stock
100 mg$518In Stock
1 mL x 10 mM (in DMSO)$68In Stock
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Purity:99.47%
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Product Introduction

Bioactivity
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]
Chemical Properties
Molecular Weight449.25
FormulaC18H17Cl2F3N4O2
Cas No.666260-75-9
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 16 mg/mL (35.6 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.2259 mL11.1297 mL22.2593 mL111.2966 mL
5 mM0.4452 mL2.2259 mL4.4519 mL22.2593 mL
10 mM0.2226 mL1.1130 mL2.2259 mL11.1297 mL
20 mM0.1113 mL0.5565 mL1.1130 mL5.5648 mL

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