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CB1 antagonist 4

Catalog No. T8511 Copy Product Info
Purity: 98.97%
🥰Excellent
CB1 antagonist 4 is an antagonist of cannabinoid receptor type 1 (CB1), with potential for the treatment of obesity and type 2 diabetes.

CB1 antagonist 4

Copy Product Info
🥰Excellent
Catalog No. T8511

CB1 antagonist 4 is an antagonist of cannabinoid receptor type 1 (CB1), with potential for the treatment of obesity and type 2 diabetes.

CB1 antagonist 4
Cas No. 1253641-65-4
Pack SizePriceUSA StockGlobal StockQuantity
2 mg$41In StockIn Stock
5 mg$98In StockIn Stock
10 mg$163In StockIn Stock
25 mg$287In StockIn Stock
50 mg$450In StockIn Stock
100 mg$663In StockIn Stock
200 mg$943-In Stock
1 mL x 10 mM (in DMSO)$166In StockIn Stock
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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For research use only—not for human use. No sales to individuals. Use as intended only.
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Purity:98.97%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
CB1 antagonist 4 is an antagonist of cannabinoid receptor type 1 (CB1), with potential for the treatment of obesity and type 2 diabetes.
In vivo
CB1 antagonist 4, a novel, largely peripherally restricted CB1 antagonist, in terms of fear-promoting consequences of systemic vs. intracerebral injections.Different groups of male C57BL/6 N mice underwent auditory fear conditioning, followed by re-exposure to the tone.Mice were treated per os (p.o.) with CB1 antagonist 4 (10, 30, or 100 mg/kg), rimonabant (10 mg/kg;a brain penetrating CB1 antagonist/inverse agonist which served as a positive control), or vehicle, 2 h prior the tone presentation.Only the high dose of CB1 antagonist 4 (100 mg/kg) induced a significant increase in freezing behavior, similar to that induced by rimonabant (10 mg/kg) (p <0.001).?If injected into the brain both CB1 antagonist 4 (10 or 30 μg/mouse) and rimonabant (1 or 10 μg/mouse) caused a sustained fear response to the tone, which was more pronounced after rimonabant treatment.Taken together, CB1 antagonist 4 was at least one order of magnitude less effective in promoting fear responses than rimonabant.Given the equipotency of the two CB1 antagonists with regard to weight loss and metabolic syndrome-like symptoms in rodent obesity models, our results point to a critical dose range in which CB1 antagonist 4 might be beneficial for indications such as obesity and metabolic disorders with limited risk of fear-promoting effects[1].
Chemical Properties
Molecular Weight617.51
FormulaC30H25Cl2F3N4OS
Cas No.1253641-65-4
SmilesCCc1c(nn(c1-c1ccc(s1)C#Cc1ccc(cc1)C(F)(F)F)-c1ccc(Cl)cc1Cl)C(=O)NN1CCCCC1
Relative Density.1.38 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 40 mg/mL (64.78 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+90% Corn Oil: 4 mg/mL (6.48 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.6194 mL8.0970 mL16.1941 mL80.9703 mL
5 mM0.3239 mL1.6194 mL3.2388 mL16.1941 mL
10 mM0.1619 mL0.8097 mL1.6194 mL8.0970 mL
20 mM0.0810 mL0.4049 mL0.8097 mL4.0485 mL
50 mM0.0324 mL0.1619 mL0.3239 mL1.6194 mL
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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