| CAS NO: | 686347-12-6 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 546.88 |
|---|---|
| Formula | C25H25Cl2N7O.HCl |
| CAS No. | 686347-12-6 (HCl); |
| 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-945,598; CP 945,598; CP-945598; Otenabant HCl; CP945598; CP 945598; CP945,598 |
| 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: Membranes are prepared from CHOK1 cells stably transfected with the human CB-1 receptor cDNA. GTPγ [35S] binding assays are performed in a 96-well FlashPlate format in duplicate using 100 pM GTPγ [35S] and 10μg membrane per well in assay buffer composed of 50 mM Tris HCl, pH 7.4, 3 mM MgCl2, pH 7.4, 10 mM MgCl2, 20 mM EGTA, 100 mM NaCl, 30 μM GDP, 0.1% bovine serum albumin, and the following protease inhibitors: 100 μg/mL bacitracin, 100 μg/mL benzamidine, 5 μg/mL aprotinin, 5 μg/mL leupeptin. The assay mix is then incubated with increasing concentrations of antagonist (10-10M to 10-5 M) for 10 min and challenged with the cannabinoid agonist CP-55,940 (10 μM). Assays are performed at 30°C for 1 h. The FlashPlates are then centrifuged at 2000 g for 10 min. Stimulation of GTPγ [35S] binding is then quantified using a Wallac Microbeta. EC50 calculations are done using Prism by GraphPad. Inverse agonism is measured in the absence of agonist. 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. |
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