CCR4 Antagonist (hydrochloride)

Chemokine (C-C motif) receptor 4 (CCR4) antagonist is an antagonist of CCR4. It inhibits activation of CCR4 by chemokine (C-C motif) ligand 22 (CCL22) in a [35S]GTPgammaS assay and also inhibits chemotaxis in human and mouse CCR4-expressing B300-19 cells (IC50s = 18, 140, and 39 nM, respectively). CCR4 antagonist inhibits microglial activation in the cortex in a mouse model of hepatic encephalopathy induced by the neurotoxin azoxymethane when administered at a dose of 1 mg/kg per day. It reduces azoxymethane-induced increases in Il6 and Il1b expression in mouse cortex. CCR4 antagonist reduces mechanical and thermal sensitivity in a mouse model of type I diabetes induced by streptozotocin (Cay-13104) when administered intrathecally at doses ranging from 10 to 30 µg/animal.Formal Name: 2-[1,4'-bipiperidin]-1'-yl-N-cycloheptyl-6,7-dimethoxy-4-quinazolinamine, dihydrochloride. CAS Number: 1784252-84-1. Synonyms: C-021. Molecular Formula: C27H41N5O2 . 2HCl. Formula Weight: 540.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 25 mg/ml, Ethanol: 5 mg/ml. lambdamax: 214, 248 nm. SMILES: COC(C(OC)=C1)=CC2=C1C(NC3CCCCCC3)=NC(N4CCC(N5CCCCC5)CC4)=N2.Cl.Cl. InChi Code: InChI=1S/C27H41N5O2.2ClH/c1-33-24-18-22-23(19-25(24)34-2)29-27(30-26(22)28-20-10-6-3-4-7-11-20)32-16-12-21(13-17-32)31-14-8-5-9-15-31,,/h18-21H,3-17H2,1-2H3,(H,28,29,30),2*1H. InChi Key: GKJKNYQUFAPLOQ-UHFFFAOYSA-N.