product name Otenabant (CP-945598) HCl
Description: Otenabant (also known as CP-945,598) HCl is a potent and highly selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, it exhibits >10,000-fold greater selectivity against human CB2 receptor. Otenabantis a drug developed by Pfizer for the treatment of obesity, but development for this drug has been discontinued due to the problems seen during clinical use of the similar drug rimonabant.
References: J Med Chem. 2009 Jan 22;52(2):234-7; Biochem Biophys Res Commun. 2010 Apr 2;394(2):366-71.
546.88
Formula
C25H25Cl2N7O.HCl
CAS No.
686347-12-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 5 mg/mL (9.1 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
0.5% methylcellulose: 17 mg/mL
Synonyms
CP-945598
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19404260
| In Vitro |
In vitro activity: CP-945598 HCl inhibits CB1 receptor with moderate unbound microsomal clearance, low hERG affinity, and adequate CNS penetration. CP-945598 HCl has low affinity with Ki of 7.6 μM for human CB2 receptors. Kinase Assay: Cell Assay: Otenabant (CP-945,598) exhibits sub-nanomolar potency at human CB1 receptors in both binding (Ki = 0.7 nM) and functional assays (Ki = 0.2 nM). The compound has low affinity (Ki = 7600 nM) for human CB2 receptors. |
|---|---|
| In Vivo | CP-945598 HCl reverses four cannabinoid agonistmediated behaviors (locomotor activity, hypothermia, analgesia, and catalepsy) following administration of the synthetic CB1 receptor agonist CP-55940. CP-945598 HCl exhibits dose-dependent anorectic activity in a model of acute food intake in rodents and increased energy expenditure and fat oxidation. CP-945598 also acutely stimulates energy expenditure in rats and decreases the respiratory quotient indicating a metabolic switch to increased fat oxidation. CP-945598 at 10 mg/kg promotes a 9%, vehicle adjusted weight loss in a 10 day weight loss study in diet-induced obese mice. |
| Animal model | Sprague-Dawley rats |
| Formulation & Dosage | Dissolved in 0.5% methyl cellulose; 30 mg/kg; p.o. administration |
| References | J Med Chem. 2009 Jan 22;52(2):234-7; Biochem Biophys Res Commun. 2010 Apr 2;394(2):366-71. |
Related Posts
product name Otenabant (CP-945598) HCl
Description: Otenabant (also known as CP-945,598) HCl is a potent and highly selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, it exhibits >10,000-fold greater selectivity against human CB2 receptor. Otenabantis a drug developed by Pfizer for the treatment of obesity, but development for this drug has been discontinued due to the problems seen during clinical use of the similar drug rimonabant.
References: J Med Chem. 2009 Jan 22;52(2):234-7; Biochem Biophys Res Commun. 2010 Apr 2;394(2):366-71.
546.88
Formula
C25H25Cl2N7O.HCl
CAS No.
686347-12-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 5 mg/mL (9.1 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
0.5% methylcellulose: 17 mg/mL
Synonyms
CP-945598
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19404260
| In Vitro |
In vitro activity: CP-945598 HCl inhibits CB1 receptor with moderate unbound microsomal clearance, low hERG affinity, and adequate CNS penetration. CP-945598 HCl has low affinity with Ki of 7.6 μM for human CB2 receptors. Kinase Assay: Cell Assay: Otenabant (CP-945,598) exhibits sub-nanomolar potency at human CB1 receptors in both binding (Ki = 0.7 nM) and functional assays (Ki = 0.2 nM). The compound has low affinity (Ki = 7600 nM) for human CB2 receptors. |
|---|---|
| In Vivo | CP-945598 HCl reverses four cannabinoid agonistmediated behaviors (locomotor activity, hypothermia, analgesia, and catalepsy) following administration of the synthetic CB1 receptor agonist CP-55940. CP-945598 HCl exhibits dose-dependent anorectic activity in a model of acute food intake in rodents and increased energy expenditure and fat oxidation. CP-945598 also acutely stimulates energy expenditure in rats and decreases the respiratory quotient indicating a metabolic switch to increased fat oxidation. CP-945598 at 10 mg/kg promotes a 9%, vehicle adjusted weight loss in a 10 day weight loss study in diet-induced obese mice. |
| Animal model | Sprague-Dawley rats |
| Formulation & Dosage | Dissolved in 0.5% methyl cellulose; 30 mg/kg; p.o. administration |
| References | J Med Chem. 2009 Jan 22;52(2):234-7; Biochem Biophys Res Commun. 2010 Apr 2;394(2):366-71. |