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CB1 antagonist 4

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Catalog No. T8511Cas No. 1253641-65-4

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

CB1 antagonist 4

🥰Excellent
Purity: 98.97%
Catalog No. T8511Cas No. 1253641-65-4
CB1 antagonist 4 is an antagonist of cannabinoid receptor type 1 (CB1), with potential for the treatment of obesity and type 2 diabetes.
Pack SizePriceAvailabilityQuantity
2 mg$41In Stock
5 mg$98In Stock
10 mg$163In Stock
25 mg$287In Stock
50 mg$450In Stock
100 mg$663In Stock
200 mg$943In Stock
1 mL x 10 mM (in DMSO)$166In Stock
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Purity:98.97%
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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 (64.77 mM), Sonication is recommended.
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

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