Basic information Safety Supplier Related
ChemicalBook >  Product Catalog >  Biochemical Engineering >  Inhibitors >  GPCR & G Protein >  Cannabinoid Receptor agonists >  GW 842166X

GW 842166X

Basic information Safety Supplier Related

GW 842166X Basic information

Product Name:
GW 842166X
Synonyms:
  • GW 842166X
  • GW 842166
  • GW842166X/GW-842166X
  • 2-(2,4-Dichlorophenylamino)-4-trifluoromethylpyrimidine-5-carboxylic acid [(tetrahydropyran-4-yl)methyl]amide
  • 2-(2,4-dichlorophenylamino)-N-((tetrahydro-2H-pyran-4-yl)methyl)-4-(trifluoromethyl)pyrimidine-5-carboxamide
  • 2-(2,4-dichloroanilino)-N-(oxan-4-ylmethyl)-4-(trifluoromethyl)pyrimidine-5-carboxamide
  • GW842166X;GW 842166
  • CS-631
CAS:
666260-75-9
MF:
C18H17Cl2F3N4O2
MW:
449.25
EINECS:
200-258-5
Product Categories:
  • Inhibitors
Mol File:
666260-75-9.mol
More
Less

GW 842166X Chemical Properties

storage temp. 
Store at -20°C
solubility 
DMF:20.0(Max Conc. mg/mL);44.52(Max Conc. mM)
DMF:PBS (pH 7.2) (1:3):0.25(Max Conc. mg/mL);0.56(Max Conc. mM)
DMSO:37.77(Max Conc. mg/mL);84.07(Max Conc. mM)
Ethanol:0.3(Max Conc. mg/mL);0.67(Max Conc. mM)
form 
Powder
color 
White to off-white
More
Less

GW 842166X Usage And Synthesis

Description

The peripheral cannabinoid (CB2) receptor is a G protein-coupled receptor (GPCR) that is localized predominantly in immune cells, monocytes, macrophages, and in several peripheral organs and binds the active component of cannabis, Δ9-tetrahydrocannabinol, as well as anandamide, an endogenous CB receptor ligand. GW 842166X is a peripheral cannabinoid (CB2) receptor agonist with ED50 values of 91 and 63 nM in rat and human, respectively. When administered orally to rats in the Freund’s complete adjuvant (FCA) model of inflammatory pain, GW 842166X is highly potent with an ED50 value of 0.1 mg/kg and full reversal of hyperalgesia at 0.3 mg/kg.

Uses

GW-842166X is pyrimidine ester based compound that is known as a highly selective CB2 receptor agonist for the treatment of inflammatory and neuropathic pain.

Definition

ChEBI: 5-pyrimidinecarboxamide, 2-[(2,4-dichlorophenyl)amino]-n-[(tetrahydro-2h-pyran-4-yl)methyl]-4-(trifluoromethyl)- is a dichlorobenzene.

in vivo

GW842166X has an oral ED50 of 0.1 mg/kg in the rat FCA model of inflammatory pain and shows full reversal of hyperalgesia at 0.3 mg/kg. The blood concentrations of GW842166X in experiments are 30 nM (0.03 mg/kg), 130 nM (0.1 mg/kg), and 370 nM (0.3 mg/ kg) 1 h after dosing. After dosing for 4 days in the FCA model, no statistical difference in antihyperalgesic response is observed on day 4 relative to day 1, indicating that tolerance does not occur[1].

References

[1] GERARD M. P. GIBLIN. Discovery of 2-[(2,4-Dichlorophenyl)amino]-N-[(tetrahydro- 2H-pyran-4-yl)methyl]-4-(trifluoromethyl)- 5-pyrimidinecarboxamide, a Selective CB2 Receptor Agonist for the Treatment of Inflammatory Pain[J]. Journal of Medicinal Chemistry, 2007, 50 11: 2597-2600. DOI: 10.1021/jm061195+
[2] RACHEL RIBEIRO . Involvement of ERK1/2, cPLA2 and NF-κB in microglia suppression by cannabinoid receptor agonists and antagonists[J]. Prostaglandins & other lipid mediators, 2013, 100: Pages 1-14. DOI: 10.1016/j.prostaglandins.2012.11.003

GW 842166XSupplier

J & K SCIENTIFIC LTD.
Tel
18210857532; 18210857532
Email
jkinfo@jkchemical.com
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
sales@meilune.com
Shanghai Aladdin Bio-Chem Technology Co.,LTD
Tel
400-6206333 13167063860
Email
anhua.mao@aladdin-e.com
MedChemexpress LLC
Tel
021-58955995
Email
sales@medchemexpress.cn
AdooQ BioScience, LLC
Tel
+1 (866) 930-6790
Email
info@adooq.com
More
Less

GW 842166X(666260-75-9)Related Product Information