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.
 |
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. |
| 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. |
| Molecular Weight | 510.42 |
| Formula | C25H25Cl2N7O |
| CAS Number | 686344-29-6 |
| Solubility (25°C) | DMSO 10 mM |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
| Related Cannabinoid Products |
|---|
| Vicasinabin
Vicasinabin (RG7774) is the potent agonist of cannabinoid receptor 2 (CB2). |
| INV-347
INV-347 is a CB1R inverse agonist that can be used in studies related to obesity. |
| RVD-Hpα TFA
RVD-Hpα TFA is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. |
| Hemopressin(human, mouse) TFA
Hemopressin TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. |
| Hemopressin(rat) TFA
Hemopressin(rat) TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
