| Name | Otenabant hydrochloride |
| Description | Otenabant hydrochloride (Otenabant) (CP-945598) is a competitive, high affinity, selective antagonist of the CB1 receptor (Ki: 0.7 nM). |
| 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. |
| 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). |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : Slightly soluble
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| Keywords | rCB1 | Otenabant hydrochloride | Inhibitor | inhibit | hCB2 | hCB1 | CP-945598 Hydrochloride | CP945598 Hydrochloride | CP-945598 | CP945598 | CP 945598 | CB | CannabinoidReceptor | Cannabinoid Receptor |
| Inhibitors Related | RTICBM-189 | β-Caryophyllene | CB2 modulator 1 | Pregnenolone | Pregnenolone acetate | CB1 antagonist 2 | Dehydroabiethylamine | CB2 receptor agonist 2 | AM-1235 | 2,3-Butanediol | Drinabant | AM281 |
| Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Membrane Protein-targeted Compound Library | ReFRAME Related Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Clinical Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |
United States
