Otenabant (CP-945598) HCl

Catalog No.S8012

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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Otenabant (CP-945598) HCl Chemical Structure

Otenabant (CP-945598) HCl Chemical Structure
Molecular Weight: 546.88

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Quality Control & MSDS

Product Information

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  • Inhibition Profile

Product Description

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]
IC50 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(Only for Reference)

Kinase Assay: [1]

CB1 GTPγ [ 35S] Binding 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: 100μg/mL bacitracin, 100μg/mL benzamidine, 5μg/mL aprotinin, 5μg/mL leupeptin. The assay mix is then incubated with increasing concentrations of antagonist (10-10 M to 10-5 M) for 10 min and challenged with the cannabinoid agonist CP-55,940 (10 μM). Assays are performed at 30 ℃ for 1 h. The FlashPlates are then centrifuged at 2000g for 10 min. Stimulation of GTPγ [35S] binding is then quantified using a Wallac Microbeta. EC50calculations are done using Prism by GraphPad. Inverse agonism is measured in the absence of agonist.

Animal Study: [2]

Animal Models Sprague-Dawley rats
Formulation In 0.5% methyl cellulose
Dosages ~30 mg/Kg
Administration p.o.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[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.

Chemical Information

Download Otenabant (CP-945598) HCl SDF
Molecular Weight (MW) 546.88


CAS No. 686347-12-6
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms Otenabant
Solubility (25°C) * In vitro DMSO 1 mg/mL warming (1.82 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
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 Name 4-Piperidinecarboxamide, 1-[8-(2-chlorophenyl)-9-(4-chlorophenyl)-9H-purin-6-yl]-4-(ethylamino)-, hydrochloride (1:1)

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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