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Otenabant (CP-945598) HCl Cannabinoid Receptor antagonist

Name: Otenabant (CP-945598) HCl
Brand: Selleck Chemicals
SKU: S8012
Availability: InStock
Rating: 5 (2 reviews)

Cat.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.

Chemical Structure

Molecular Weight: 546.88

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

99.80

Related Targets	CXCR Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas
Other Cannabinoid Receptor Inhibitors	AM1241 AM251 BML-190 Org 27569 6-Iodopravadoline (AM630) GW842166X CID16020046 WIN 55, 212-2 mesylate Pregnenolone monosulfate sodium RTICBM-189

Solubility

In vitro
Batch:

4-Methylpyridine : 5 mg/mL

DMSO : 1 mg/mL (1.82 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	0.5% methylcellulose Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	10.000mg/ml (18.29mM)	Taking the 1 mL working solution as an example, take 10 mg of this product, add it to 1 ml of 0.5% methylcellulose clear solution, and mix evenly to form a uniform suspension. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

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Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	546.88	Formula	C₂₅H₂₅Cl₂N₇O.HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	686347-12-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Otenabant			Smiles	CCNC1(CCN(CC1)C2=NC=NC3=C2N=C(N3C4=CC=C(C=C4)Cl)C5=CC=CC=C5Cl)C(=O)N.Cl

Mechanism of Action

Targets/IC₅₀/Ki	hCB1 0.7 nM(Ki) rCB1 2.8 nM(Ki)
In vitro	CP-945598 HCl inhibits CB₁ receptor with moderate unbound microsomal clearance, low hERG affinity, and adequate CNS penetration. CP-945598 HCl has low affinity with K_i of 7.6 μM for human CB₂ receptors.
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. 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.
References	[1] http://www.ncbi.nlm.nih.gov/pubmed/?term=19102698 [2] http://www.ncbi.nlm.nih.gov/pubmed/?term=20211605

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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