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Otenabant hydrochloride

Catalog No. T1796 CAS 686347-12-6

Synonyms: Otenabant (CP-945598) HCl, CP 945598 Hydrochloride, Otenabant

Otenabant hydrochloride (Otenabant) (CP-945598) is a competitive, high affinity, selective antagonist of the CB1 receptor (Ki: 0.7 nM).

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Otenabant hydrochloride Chemical Structure

Otenabant hydrochloride, CAS 686347-12-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 39.00
2 mg	In stock	$ 54.00
5 mg	In stock	$ 74.00
10 mg	In stock	$ 123.00
25 mg	In stock	$ 252.00
50 mg	In stock	$ 466.00
100 mg	In stock	$ 683.00

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Purity: 99.79%

Purity: 99.52%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Otenabant hydrochloride (Otenabant) (CP-945598) is a competitive, high affinity, selective antagonist of the CB1 receptor (Ki: 0.7 nM).
Targets&IC50	CB1 (rat):2.8 nM(Ki), CB1 (human):0.7 nM(Ki)
In vitro	In a diet-induced obesity model in mice, CP-945598 (10 mg/kg) facilitated a 9% reduction in body weight over a 10-day weight loss study. CP-945598 significantly enhanced energy expenditure in rats and reduced the respiratory quotient, indicating a metabolic shift towards increased fat oxidation. Additionally, CP-945598 HCl reversed behaviors mediated by four cannabinoid agonists (hypothermia, spontaneous activity, catalepsy, and analgesia). In acute food intake models in rodent species, CP-945598 HCl suppressed appetite, further promoting fat oxidation and energy consumption.
In vivo	CP-945598 HCl exhibits lower affinity towards human CB2 receptors (Ki: 7.6 μM) and demonstrates inhibitory effects on the CB1 receptor. Additionally, it possesses moderate microsomal clearance, low affinity for hERG, and sufficient penetration of the central nervous system (CNS).
Kinase Assay	Membranes are prepared from CHOK1 cells stably transfected with the human CB-1 receptor cDNA. GTPγ [35S] binding assays are performed in a 96-well FlashPlate format in duplicate using 100 pM GTPγ [35S] and 10μg membrane per well in assay buffer composed of 50 mM Tris HCl, pH 7.4, 3 mM MgCl2, pH 7.4, 10 mM MgCl2, 20 mM EGTA, 100 mM NaCl, 30 μM GDP, 0.1% bovine serum albumin, and the following protease inhibitors: 100 μg/mL bacitracin, 100 μg/mL benzamidine, 5 μg/mL aprotinin, 5 μg/mL leupeptin. The assay mix is then incubated with increasing concentrations of antagonist (10-10M to 10-5 M) for 10 min and challenged with the cannabinoid agonist CP-55,940 (10 μM). Assays are performed at 30°C for 1 h. The FlashPlates are then centrifuged at 2000 g for 10 min. Stimulation of GTPγ [35S] binding is then quantified using a Wallac Microbeta. EC50 calculations are done using Prism by GraphPad. Inverse agonism is measured in the absence of agonist.

Synonyms	Otenabant (CP-945598) HCl, CP 945598 Hydrochloride, Otenabant
Molecular Weight	546.88
Formula	C25H26Cl3N7O
CAS No.	686347-12-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: Slightly soluble

References and Literature

1. Griffith DA, et al. J Med Chem, 2009, 52(2), 234-237. 2. Hadcock JR, et al. Biochem Biophys Res Commun, 2010, 394(2), 366-371.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Neurodegenerative Disease Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library GPCR Compound Library Inhibitor Library Highly Selective Inhibitor Library Drug Repurposing Compound Library Bioactive Compounds Library Max Anti-Fibrosis Compound Library Clinical Compound Library

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Keywords

Otenabant hydrochloride 686347-12-6 GPCR/G Protein Cannabinoid Receptor CP945598 Otenabant (CP-945598) HCl inhibit CP945598 Hydrochloride CP 945598 Hydrochloride Inhibitor CP-945598 Hydrochloride CP 945598 Otenabant CP-945598 Otenabant Hydrochloride inhibitor

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