[CAS NO. 686347-12-6] Otenabant (CP-945598) HCl

Name: Otenabant (CP-945598) HCl
Brand: Arctom Scientific
SKU: SLK-S8012

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PRODUCTS SPECIFICATIONS [686347-12-6]

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Catalog

SLK-S8012

Brand

Selleck

CAS

686347-12-6

DESCRIPTION [686347-12-6]

Overview

MDL	-
Molecular Weight	546.88
Molecular Formula	C25H25Cl2N7O.HCl
SMILES	ClC1=C(C=2N(C=3C(N2)=C(N=CN3)N4CCC(NCC)(C(N)=O)CC4)C5=CC=C(Cl)C=C5)C=CC=C1.Cl

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.8286 mL	9.1428 mL	18.2855 mL
5 mM	0.3657 mL	1.8286 mL	3.6571 mL
10 mM	-	-	-
50 mM	-	-	-

Description

Otenabant (CP-945598) HCl is a potent and selective antagonist with of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor. Phase 1.

Targets

hCB1 ^[1]	rCB1 ^[2]
0.7 nM(Ki)	2.8 nM(Ki)

In vitro

CP-945598 HCl inhibits CB receptor with moderate unbound microsomal clearance, low hERG affinity, and adequate CNS penetration. CP-945598 HCl has low affinity with K of 7.6 μM for human CB receptors.

In vivo

CP-945598 HCl reverses four cannabinoid agonistmediated behaviors (locomotor activity, hypothermia, analgesia, and catalepsy) following administration of the synthetic CB 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] 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.

Synonyms

4-Piperidinecarboxamide, 1-[8-(2-chlorophenyl)-9-(4-chlorophenyl)-9H-purin-6-yl]-4-(ethylamino)-, hydrochloride (1:1)

4-Piperidinecarboxamide, 1-[8-(2-chlorophenyl)-9-(4-chlorophenyl)-9H-purin-6-yl]-4-(ethylamino)-, monohydrochloride

Otenabant hydrochloride

CP 945598

CP 945598-01