Otenabant (CP-945598) HCl

Catalog No.S8012 Synonyms: Otenabant

Otenabant (CP-945598) HCl Chemical Structure

Molecular Weight(MW): 546.88

Otenabant (CP-945598) HCl is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor. Phase 1.

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description Otenabant (CP-945598) HCl is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor. Phase 1.
Targets
hCB1 [1] rCB1 [2] hCB2 [2]
0.7 nM(Ki) 2.8 nM(Ki) 7.663 μM(Ki)
In vitro

CP-945598 HCl inhibits CB1 receptor with moderate unbound microsomal clearance, low hERG affinity, and adequate CNS penetration. [1] CP-945598 HCl has low affinity with Ki of 7.6 μM for human CB2 receptors. [2]

In vivo CP-945598 HCl reverses four cannabinoid agonistmediated behaviors (locomotor activity, hypothermia, analgesia, and catalepsy) following administration of the synthetic CB1 receptor agonist CP-55940. CP-945598 HCl exhibits dose-dependent anorectic activity in a model of acute food intake in rodents and increased energy expenditure and fat oxidation. [1] CP-945598 also acutely stimulates energy expenditure in rats and decreases the respiratory quotient indicating a metabolic switch to increased fat oxidation. CP-945598 at 10 mg/kg promotes a 9%, vehicle adjusted weight loss in a 10 day weight loss study in diet-induced obese mice. [2]

Protocol

Animal Research
+ Expand
  • Animal Models: Sprague-Dawley rats
  • Formulation: In 0.5% methyl cellulose
  • Dosages: ~30 mg/Kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 5 mg/mL (9.14 mM) warming
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 0.5% methylcellulose 17 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 546.88
Formula

C25H25Cl2N7O.HCl

CAS No. 686347-12-6
Storage powder
in solvent
Synonyms Otenabant

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Cannabinoid Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID