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CP 945598

Cat. No. M2552
CP 945598 Structure
Synonym:

Otenabant, CP945598

Size Price Availability Quantity
10mM*1mL In DMSO USD 90 In stock
10mg USD 120 In stock
50mg USD 430 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

CP 945598 (Otenabant) is a potent and selective cannabinoid type 1 receptor antagonist that inhibits both basal and cannabinoid agonist-mediated CB(1) receptor signaling in vitro and in vivo. CP-945598 exhibits sub-nanomolar potency at human CB1 receptors in both binding (Ki = 0.7 nM) and functional assays (Ki = 0.2 nM) in vitro. CP-945598 (Otenabant) also acutely stimulates energy expenditure in rats and decreases the respiratory quotient indicating a metabolic switch to increased fat oxidation. A phase 1 study with CP-945598 of the roles of endocannabinoids in insulin secretion and action is recruiting.

Customer Product Validations & Biological Datas
Source Drug Metab Dispos (2011). Figure 3. CP 945598
Method oral administration
Cell Lines rats
Concentrations 30 mg/kg
Incubation Time -
Results Mean serum concentration-time curves for unchanged CP-945,598, M1, and total radioactivity are shown in Fig. 3 for both male and female rats, respectively.
Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Sprague-Dawley rats
Formulation In 0.5% methyl cellulose
Dosages ~30 mg/Kg
Administration p.o.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 510.42
Formula C25H25Cl2N7O
CAS Number 686344-29-6
Purity >98%
Solubility DMSO
Storage at -20°C
References

Excretion, metabolism, and pharmacokinetics of CP-945,598, a selective cannabinoid receptor antagonist, in rats, mice, and dogs.
Miao Z, et al. Drug Metab Dispos. 2011 Dec;39(12):2191-208. PMID: 21875952.

In vitro and in vivo pharmacology of CP-945,598, a potent and selective cannabinoid CB(1) receptor antagonist for the management of obesity.
Hadcock JR, et al. Biochem Biophys Res Commun. 2010 Apr 2;394(2):366-71. PMID: 20211605.

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  Catalog
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Keywords: CP 945598, Otenabant, CP945598 supplier, Cannabinoid, inhibitors

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