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 5 mg/mL warming (9.14 mM)
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 Name 4-Piperidinecarboxamide, 1-[8-(2-chlorophenyl)-9-(4-chlorophenyl)-9H-purin-6-yl]-4-(ethylamino)-, hydrochloride (1:1)

Tech Support

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