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Otenabant

Catalog No. T3530 CAS 686344-29-6

Synonyms: CP-945598

Otenabant has been investigated for the treatment of Obesity.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Otenabant, CAS 686344-29-6

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Otenabant has been investigated for the treatment of Obesity.
Targets&IC50	cannabinoid:0.7 nM(Ki)
In vitro	Otenabant HCl has a low Ki affinity for human CB2 receptors of 7.6 μM[1]. Otenabant HCl inhibits CB1 receptor with moderate unbound microsomal clearance, low hERG affinity, and adequate CNS penetration[2].
In vivo	Otenabant acutely stimulates energy expenditure in rats and decreases the respiratory quotient which suggests 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[1]. Otenabant HCl reverses four cannabinoid agonist-mediated 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[2].

Synonyms	CP-945598
Molecular Weight	510.42
Formula	C25H25Cl2N7O
CAS No.	686344-29-6

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: <10 mg/mL (19.59 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. John R. Hadcock, et al. In vitro and in vivo pharmacology of CP-945,598, a potent and selective cannabinoid CB1 receptor antagonist for the management of obesity. Biochemical and Biophysical Research Communications, 2010; 394;366-371. 2. Griffith DA, et al. Discovery of 1-[9-(4-chlorophenyl) -8-(2-chlorophenyl)- 9H-purin-6-yl] -4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist. JMedChem. 2009 ;5

Citations

1. Li P, Lin Q, Sun S, et al. Inhibition of cannabinoid receptor type 1 sensitizes triple-negative breast cancer cells to ferroptosis via regulating fatty acid metabolism. Cell Death & Disease. 2022, 13(9): 1-15.

Dose Conversion

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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 add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Otenabant 686344-29-6 GPCR/G Protein Cannabinoid Receptor inhibit CP 945598 CP-945598 Inhibitor CP945598 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.