Otenabant hydrochloride

SKU: orb1224244

Description

A potent, and selective CB1 receptor antagonist with Ki of 0.7 nM/0.12 nM in binding and functional assays respectively; has low affinity (Ki=7600 nM) for human CB2 receptors; reverses cannabinoid agonist mediated responses, reduces food intake, and increases energy expenditure and fat oxidation in rodents.Obesity Phase 3 Discontinued(In Vitro):Otenabant HCl has low affinity with Ki of 7.6 μM for human CB2 receptors. Otenabant HCl inhibits CB1 receptor with moderate unbound microsomal clearance, low hERG affinity, and adequate CNS penetration.(In Vivo):Otenabant 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. Otenabant HCl reverses four cannabinoid agonistmediated behaviors (locomotor activity, hypothermia, analgesia, and catalepsy) following administration of the synthetic CB1 receptor agonist CP-55940. Otenabant HCl exhibits dose-dependent anorectic activity in a model of acute food intake in rodents and increased energy expenditure and fat oxidation.

Key Properties

• CAS Number: 686347-12-6
• MW: 546.8792
• Purity: >98% (HPLC)
• Formula: C₂₅H₂₆Cl₃N₇O
• SMILES: CCNC1(CCN(CC1)C1=NC=NC2=C1NC(N2C1=CC=C(Cl)C=C1)C1=CC=CC=C1Cl)C(N)=O
• Target: Cannabinoid Receptor
• Solubility: DMSO: 1 mg/mL

Bioactivity

• In Vivo:
  Otenabant 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. Otenabant HCl reverses four cannabinoid agonistmediated behaviors (locomotor activity, hypothermia, analgesia, and catalepsy) following administration of the synthetic CB1 receptor agonist CP-55940. Otenabant HCl exhibits dose-dependent anorectic activity in a model of acute food intake in rodents and increased energy expenditure and fat oxidation.
• In Vitro:
  Otenabant HCl has low affinity with Ki of 7.6 μM for human CB2 receptors. Otenabant HCl inhibits CB1 receptor with moderate unbound microsomal clearance, low hERG affinity, and adequate CNS penetration.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CP 945598 Hydrochloride | CP-945598 Hydrochloride | CP945598 Hydrochloride

Quick Database Links

Gene Symbol

Cannabinoid Receptor