GW842166X

Catalog No.S2778

GW842166X Chemical Structure

Molecular Weight(MW): 449.25

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.

Size Price Stock Quantity  
In DMSO USD 200 In stock
USD 110 In stock
USD 170 In stock
USD 270 In stock
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Biological Activity

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.
Features Possesses selective affinity for CB2 than CB1.
Targets
CB2 [1]
63 nM(EC50)
In vitro

GW842166X shows similar potency and efficacy for rat and human recombinant CB2 receptors with EC50 of 91 nM and 63nM, 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]

Protocol

Animal Research:[3]
+ Expand
  • Animal Models: rat model of neuropathic pain
  • Formulation: saline
  • Dosages: 15 mg/kg
  • Administration: Orally administrated once daily for 8 days
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 20 mg/mL (44.51 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% propylene glycol, 5% Tween 80, 65% D5W
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 449.25
Formula

C18H17Cl2F3N4O2

CAS No. 666260-75-9
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00554762 Withdrawn Healthy Subjects GlaxoSmithKline November 2007 Phase 1
NCT00554762 Withdrawn Healthy Subjects GlaxoSmithKline November 2007 Phase 1
NCT00536497 Withdrawn Healthy Subjects GlaxoSmithKline September 2007 Phase 1
NCT00536497 Withdrawn Healthy Subjects GlaxoSmithKline September 2007 Phase 1
NCT00511524 Completed Pain Inflammatory GlaxoSmithKline June 26 2007 Phase 1
NCT00511524 Completed Pain Inflammatory GlaxoSmithKline June 26 2007 Phase 1

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cannabinoid Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID