GW 842166X

GW 842166X is a cannabinoid 2 (CB2) receptor agonist. It increases intracellular calcium mobilization induced by the CB receptor agonist CP 55,940 (Cay-13241) in HEK cells co-expressing a chimeric Galphaq/05 protein and the human CB2 receptor (EC50 = 7.78 µM). GW 842166X is selective for CB2 over the CB1 receptor (IC50s = 0.133 and >25 µM, respectively). It inhibits LPS-induced production of inducible nitric oxide synthase (iNOS), as well as reduces LPS-induced phosphorylation of ERK1/2 in BV-2 microglia cells when used at a concentration of 100 nM. GW 842166X inhibits hyperalgesia in a rat model of inflammatory pain induced by complete Freund's adjuvant (ED50 = 0.1 mg/kg).Formal Name: 2-[(2,4-dichlorophenyl)amino]-N-[(tetrahydro-2H-pyran-4-yl)methyl]-4-(trifluoromethyl)-5-pyrimidinecarboxamide. CAS Number: 666260-75-9. Molecular Formula: C18H17Cl2F3N4O2. Formula Weight: 449.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMF:PBS (pH 7.2) (1:3): 0.25 mg/ml, DMSO: 10 mg/ml, Ethanol: 0.3 mg/ml. lambdamax: 280 nm. SMILES: Clc1ccc(Nc2ncc(C(=O)NCC3CCOCC3)c(n2)C(F)(F)F)c(Cl)c1. InChi Code: InChI=1S/C18H17Cl2F3N4O2/c19-11-1-2-14(13(20)7-11)26-17-25-9-12(15(27-17)18(21,22)23)16(28)24-8-10-3-5-29-6-4-10/h1-2,7,9-10H,3-6,8H2,(H,24,28)(H,25,26,27). InChi Key: TWQYWUXBZHPIIV-UHFFFAOYSA-N.