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

| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 2 mg | $41 | In Stock | In Stock | |
| 5 mg | $98 | In Stock | In Stock | |
| 10 mg | $163 | In Stock | In Stock | |
| 25 mg | $287 | In Stock | In Stock | |
| 50 mg | $450 | In Stock | In Stock | |
| 100 mg | $663 | In Stock | In Stock | |
| 200 mg | $943 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $166 | In Stock | In Stock |
| 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]. |
| Molecular Weight | 617.51 |
| Formula | C30H25Cl2F3N4OS |
| Cas No. | 1253641-65-4 |
| Smiles | CCc1c(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 | Powder: -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
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. | |||||||||||||||||||||||||||||||
Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
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 ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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