Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Otenabant hydrochloride (Otenabant) (CP-945598) is a competitive, high affinity, selective antagonist of the CB1 receptor (Ki: 0.7 nM).
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1 mg | 在庫あり | ¥ 9,000 | |||
2 mg | 在庫あり | ¥ 12,500 | |||
5 mg | 在庫あり | ¥ 17,000 | |||
10 mg | 在庫あり | ¥ 28,500 | |||
25 mg | 在庫あり | ¥ 58,000 | |||
50 mg | 在庫あり | ¥ 107,000 | |||
100 mg | 在庫あり | ¥ 157,000 |
説明 | Otenabant hydrochloride (Otenabant) (CP-945598) is a competitive, high affinity, selective antagonist of the CB1 receptor (Ki: 0.7 nM). |
ターゲット&IC50 | CB1 (rat):2.8 nM(Ki), CB1 (human):0.7 nM(Ki) |
In vitro | In a diet-induced obesity model in mice, CP-945598 (10 mg/kg) facilitated a 9% reduction in body weight over a 10-day weight loss study. CP-945598 significantly enhanced energy expenditure in rats and reduced the respiratory quotient, indicating a metabolic shift towards increased fat oxidation. Additionally, CP-945598 HCl reversed behaviors mediated by four cannabinoid agonists (hypothermia, spontaneous activity, catalepsy, and analgesia). In acute food intake models in rodent species, CP-945598 HCl suppressed appetite, further promoting fat oxidation and energy consumption. |
In vivo | CP-945598 HCl exhibits lower affinity towards human CB2 receptors (Ki: 7.6 μM) and demonstrates inhibitory effects on the CB1 receptor. Additionally, it possesses moderate microsomal clearance, low affinity for hERG, and sufficient penetration of the central nervous system (CNS). |
キナーゼ試験 | 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. |
別名 | Otenabant (CP-945598) HCl, CP 945598 Hydrochloride, Otenabant |
分子量 | 546.88 |
分子式 | C25H26Cl3N7O |
CAS No. | 686347-12-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: Slightly soluble
You can also refer to dose conversion for different animals. 詳細
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