Home GPCR & G Protein Cannabinoid Receptor agonist GW842166X For research use only.

GW842166X

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 Chemical Structure

GW842166X Chemical Structure

CAS No. 666260-75-9

Purity & Quality Control

GW842166X Related Products

Signaling Pathway

Cannabinoid Receptor Signaling Pathways

Cannabinoid Receptor Signaling Pathway

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
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]
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-Met / Met 28164434
Immunofluorescence p-EGFR 30390071
Growth inhibition assay Cell viability 28164434
In Vivo
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]
Animal Research Animal Models rat model of neuropathic pain
Dosages 15 mg/kg
Administration Orally administrated once daily for 8 days

Chemical Information & Solubility

Molecular Weight 449.25 Formula

C18H17Cl2F3N4O2
CAS No. 666260-75-9 SDF Download GW842166X SDF
Smiles C1COCCC1CNC(=O)C2=CN=C(N=C2C(F)(F)F)NC3=C(C=C(C=C3)Cl)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 20 mg/mL ( (44.51 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Tech Support

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.

Handling Instructions

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