[CAS NO. 666260-75-9] GW842166X

Name: GW842166X
Brand: Arctom Scientific
SKU: SLK-S2778

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PRODUCTS SPECIFICATIONS [666260-75-9]

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Catalog

SLK-S2778

Brand

Selleck

CAS

666260-75-9

DESCRIPTION [666260-75-9]

Overview

MDL	-
Molecular Weight	449.25
Molecular Formula	C18H17Cl2F3N4O2
SMILES	C(NCC1CCOCC1)(=O)C=2C(C(F)(F)F)=NC(NC3=C(Cl)C=C(Cl)C=C3)=NC2

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	2.2259 mL	11.1297 mL	22.2593 mL
5 mM	0.4452 mL	2.2259 mL	4.4519 mL
10 mM	0.2226 mL	1.1130 mL	2.2259 mL
50 mM	-	-	-

Description

GW842166X is a potent and highly selective agonist of receptor with of 63 nM, shows no significant activity at CB1 receptor. Phase 2.

Features

Possesses selective affinity for CB2 than CB1.

Targets

CB2 ^[1]

63 nM(EC50)

In vitro

GW842166X shows similar potency and efficacy for rat and human recombinant CB2 receptors with EC50 of 91 nM and 63nM, respectively. GW-842166X exhibits full agonist potency with an EC50 of 133 nM and E of 101% in cyclase assays. GW-842166X exhibits weak agonist potency with an EC50 of 7.780 μM and E of 84% in FLIPR assays.

In vivo

GW842166X has an oral bioavailability of 58% and a half-life of 3 h when dosed orally in the rat. GW842166X has extremely high potency with an oral ED50 of 0.1 mg/kg and shows full reversal of hyperalgesia at 0.3 mg/kg in the FCAa model of inflammatory pain. GW842166X orally administrated at a dose of 15 mg/kg for 8 days produced a significant reversal of the CCI induced decrease in paw withdrawal threshold in a rat model of neuropathic pain.

References

[1] Giblin GM, et al. J Med Chem, 2007, 50(11), 2597-2600.
[2] Yao BB, et al. Br J Pharmacol, 2008, 153(2), 390-401.

Synonyms

5-Pyrimidinecarboxamide, 2-[(2,4-dichlorophenyl)amino]-N-[(tetrahydro-2H-pyran-4-yl)methyl]-4-(trifluoromethyl)-

2-[(2,4-Dichlorophenyl)amino]-N-[(tetrahydro-2H-pyran-4-yl)methyl]-4-(trifluoromethyl)-5-pyrimidinecarboxamide

2-(2,4-Dichlorophenylamino)-4-trifluoromethylpyrimidine-5-carboxylic acid [(tetrahydropyran-4-yl)methyl]amide

GW 842166X

GW 842166

2-(2,4-Dichloroanilino)-N-(oxan-4-ylmethyl)-4-(trifluoromethyl)pyrimidine-5-carboxamide