Home GPCR & G Protein Cannabinoid Receptor antagonist Otenabant (CP-945598) HCl For research use only.

Otenabant (CP-945598) HCl

Synonyms: Otenabant

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.

Otenabant (CP-945598) HCl Chemical Structure

Otenabant (CP-945598) HCl Chemical Structure

CAS No. 686347-12-6

Purity & Quality Control

Batch: S801201 4-Methylpyridine]5 mg/mL]true]DMSO]1 mg/mL]false]Water]Insoluble]false Purity: 99.80%
99.80

Otenabant (CP-945598) HCl Related Products

Signaling Pathway

Cannabinoid Receptor Signaling Pathways

Cannabinoid Receptor Signaling Pathway

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]
0.7 nM(Ki) 2.8 nM(Ki)
In vitro
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
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]
Animal Research Animal Models Sprague-Dawley rats
Dosages ~30 mg/Kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00706537 Completed
Non-Alcoholic Steatohepatitis(NASH)
Pfizer
 July 2008 Phase 1
NCT00644839 Completed
Obesity
Pfizer
 April 2008 Phase 1
NCT00645463 Completed
Obesity
Pfizer
 March 2007 Phase 1
NCT00134199 Completed
Obesity
Pfizer
 March 2005 Phase 2|Phase 3

Chemical Information & Solubility

Molecular Weight 546.88 Formula

C25H25Cl2N7O.HCl
CAS No. 686347-12-6 SDF Download Otenabant (CP-945598) HCl SDF
Smiles CCNC1(CCN(CC1)C2=NC=NC3=C2N=C(N3C4=CC=C(C=C4)Cl)C5=CC=CC=C5Cl)C(=O)N.Cl
Storage (From the date of receipt)

In vitro
Batch:

4-Methylpyridine : 5 mg/mL

DMSO : 1 mg/mL ( (1.82 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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