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

Size Price Stock Quantity
10mM (1mL in DMSO) USD 200 In stock
5mg USD 110 In stock
10mg USD 170 In stock
25mg USD 270 In stock
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Selleck's GW842166X has been cited by 1 publication

Purity & Quality Control

GW842166X Related Products

Signaling Pathway

Cannabinoid Receptor Signaling Pathways

Cannabinoid Receptor Signaling Pathway

Choose Selective Cannabinoid Receptor Inhibitors

Name Citation CB1 CB2
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JD-5037 0
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AM251
Pregnenolone monosulfate sodium
1. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation. 2. "✔" indicates inhibitory effect, but without specific value.

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


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator
Clear solution
5%DMSO 40% 5% 50%ddH2O
1.0mg/ml (2.23mM) Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 

Preparing Stock Solutions

1 mg 5 mg 10 mg
1 mM 2.2259 mL 11.1297 mL 22.2593 mL
5 mM 0.4452 mL 2.2259 mL 4.4519 mL
10 mM 0.2226 mL 1.1130 mL 2.2259 mL
50 mM - - -

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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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