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GW842166X

SKU: orb1300691

Description

GW842166X is a potent and selective CB2 receptor agonist (EC50 = 63 nM) with negligible activity at CB1. It has been investigated in Phase 2 clinical trials and is a valuable research tool for studying CB2 function in inflammatory and neuropathic pain models, both in vitro and in vivo.

Research Area

Pharmacology & Drug Discovery

Images & Validation

Key Properties

CAS Number666260-75-9
MW449.25
Purity99.88%
FormulaC18H17Cl2F3N4O2
SMILESFC(F)(F)c1nc(Nc2cc(Cl)cc(Cl)c2)ncc1C(=O)NCC1CCOCC1
TargetCannabinoid Receptor
SolubilityH2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:16 mg/mL (35.61 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

Target IC50
CB2:63 nM(EC50)
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. 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.
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. 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%.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

CB2, CB, Cannabinoid Receptor, CannabinoidReceptor, GW842166X, GW-842166X, Inhibitor, inhibit

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    >98% (HPLC)

    666260-75-9

    449.3

    C18H17Cl2F3N4O2

    1 g, 500 mg, 200 mg, 50 mg, 100 mg, 5 mg, 10 mg, 25 mg, 2 mg
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Key Properties

No computed properties available.

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Protocol Information

GW842166X (orb1300691)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

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1 ml x 10 mM (in DMSO)
$ 90.00
5 mg
$ 90.00
10 mg
$ 120.00
25 mg
$ 190.00
50 mg
$ 250.00
100 mg
$ 340.00
200 mg
$ 460.00
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