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CP-945598 HCl

Catalog No.
A1435
CB1 antagonist,selective and high affinity
Grouped product items
SizePriceStock Qty
5mg
$50.00
In stock
25mg
$150.00
In stock
100mg
$480.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

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Background

CP 945598 hydrochloride is a selective and high affinity CB1 antagonist with Ki value of 0.7 and 0.12 nM for binding and functional assays, respectively [1].
The CB1 receptor is a G protein-coupled cannabinoid receptor located primarily in the central and peripheral nervous system and plays an important role in energy homeostasis.
CP 945598 dose-dependently reversed the four characteristic effects (hypothermia, anti-nociception, hypo-locomotion, and catalepsy) of a centrally acting cannabinoid agonist (CP 55940).
In mice model, CP 945598 (17.8 mg/kg s.c.) increased locomotor activity. In Sprague–
Dawley rats, CP 945598 reduced food intake in a dose and concentration dependent way. With doses of 10 mg/kg and 30 mg/kg, CP 945598 increased energy expenditure by 16% and 19%, respectively. Also, ex vivo brain receptor occupancy increased to 33–36% in a dose-related way. In diet-induced obese mice, CP 945598 significantly decreased body weight by 9% compared to vehicle-treated mice [2].
References:
[1]. Griffith DA, Hadcock JR, Black SC, 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. J Med Chem, 2009, 52(2): 234-237.
[2]. Hadcock JR1, Griffith DA, Iredale PA, 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. Biochem Biophys Res Commun, 2010, 394(2): 366-371.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt546.88
Cas No.686347-12-6
FormulaC25H25Cl2N7O·HCl
Solubility≥27.35 mg/mL in DMSO with gentle warming; insoluble in H2O; insoluble in EtOH
Chemical Name1-[8-(2-chlorophenyl)-9-(4-chlorophenyl)purin-6-yl]-4-(ethylamino)piperidine-4-carboxamide;hydrochloride
SDFDownload SDF
Canonical SMILESCCNC1(CCN(CC1)C2=NC=NC3=C2N=C(N3C4=CC=C(C=C4)Cl)C5=CC=CC=C5Cl)C(=O)N.Cl
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Biological Activity

Description CP-945598 HCl is a selective and high affinity antagonist of CB1 with Ki value of 0.7 nM.
Targets CB1 CB2        
IC50 0.7 nM (Ki) 7.6 μM (Ki)        

Quality Control

Quality Control & MSDS

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Chemical structure

CP-945598 HCl