2. GPCR/G Protein Neuronal Signaling
  3. Cannabinoid Receptor
  4. GW842166X

GW842166X is a potent and selective cannabinoid receptor 2 (CB2) agonist with IC50 values of 63 and 91 nM for human and rat CB2, respectively.

For research use only. We do not sell to patients.

GW842166X Chemical Structure

GW842166X Chemical Structure

CAS No. : 666260-75-9

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 87 In-stock
Solution
10 mM * 1 mL in DMSO USD 87 In-stock
Solid
2 mg USD 55 In-stock
5 mg USD 88 In-stock
10 mg USD 154 In-stock
25 mg USD 286 In-stock
50 mg   Get quote  
100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

GW842166X Related Antibodies

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Description

GW842166X is a potent and selective cannabinoid receptor 2 (CB2) agonist with IC50 values of 63 and 91 nM for human and rat CB2, respectively.

IC50 & Target

IC50: 63 nM (human CB2), 91 nM (rat CB2)[1]
In Vitro

GW842166X shows similar potency and efficacy for rat and human recombinant CB2 receptors. It has no significant agonist activity at concentrations up to 30 µM in human and rat CB1 recombinant assays[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GW842166X Related Antibodies
In Vivo

GW842166X has an oral ED50 of 0.1 mg/kg in the rat FCA model of inflammatory pain and shows full reversal of hyperalgesia at 0.3 mg/kg. The blood concentrations of GW842166X in experiments are 30 nM (0.03 mg/kg), 130 nM (0.1 mg/kg), and 370 nM (0.3 mg/ kg) 1 h after dosing. After dosing for 4 days in the FCA model, no statistical difference in antihyperalgesic response is observed on day 4 relative to day 1, indicating that tolerance does not occur[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

449.25

Formula

C18H17Cl2F3N4O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC(Cl)=C(NC2=NC=C(C(NCC3CCOCC3)=O)C(C(F)(F)F)=N2)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 83.3 mg/mL (185.42 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (5.56 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.56 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.97%

COA (246 KB) HNMR (207 KB) LCMS (406 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2259 mL 11.1297 mL 22.2593 mL 55.6483 mL
5 mM 0.4452 mL 2.2259 mL 4.4519 mL 11.1297 mL
10 mM 0.2226 mL 1.1130 mL 2.2259 mL 5.5648 mL
15 mM 0.1484 mL 0.7420 mL 1.4840 mL 3.7099 mL
20 mM 0.1113 mL 0.5565 mL 1.1130 mL 2.7824 mL
25 mM 0.0890 mL 0.4452 mL 0.8904 mL 2.2259 mL
30 mM 0.0742 mL 0.3710 mL 0.7420 mL 1.8549 mL
40 mM 0.0556 mL 0.2782 mL 0.5565 mL 1.3912 mL
50 mM 0.0445 mL 0.2226 mL 0.4452 mL 1.1130 mL
60 mM 0.0371 mL 0.1855 mL 0.3710 mL 0.9275 mL
80 mM 0.0278 mL 0.1391 mL 0.2782 mL 0.6956 mL
100 mM 0.0223 mL 0.1113 mL 0.2226 mL 0.5565 mL
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GW842166X Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GW842166X666260-75-9Cannabinoid ReceptorInhibitorinhibitorinhibit

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