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Otenabant (CP-945598) 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.
Otenabant (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. Otenabant (CP-945598) also acutely stimulates energy expenditure in rats and decreases the respiratory quotient indicating a metabolic switch to increased fat oxidation.
Otenabant (10 mg/kg, p.o.) promotes a 9%, vehicle adjusted weight loss in a 10 day weight loss study in diet-induced obese mice.
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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 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Cannabinoid Products |
|---|
| Org 27569
Org 27569 is a potent and selective allosteric modulator of the cannabinoid CB1 receptor. |
| AM1241
AM1241 is a cannabinoid CB2 receptor selective agonist. |
| CP 945598 hydrochloride
CP 945598 hydrochloride is a selective and high affinity CB1 antagonist (Ki values are 0.7 and 0.12 nM in binding and functional assays respectively). |
| AM-2201
AM-2201 is a potent synthetic cannabinoid (CB) with Ki values of 1.0 and 2.6 nM for the CB1 and CB2 receptors, respectively. |
| AM251
AM251 block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain. |
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