INCB 3284 (dimesylate)

CCR2 is the receptor for the chemokine CCL2, known commonly as monocyte chemotactic protein-1 (MCP-1). INCB 3284 is a potent, selective, and orally bioavailable antagonist of monocyte chemotactic protein-1 binding to CCR2 (IC50 = 3.7 nM). For comparison, it has no significant inhibitor action at over 50 ion channels, transporters, GPCRs, and other chemokine receptors when tested at a concentration of 1 µM. INCB 3284 inhibits chemotaxis in vitro (IC50 = 4.7 nM) and displays acceptable oral bioavailability in mice, rats, dogs, monkeys, and chimpanzees.Formal Name: N-[2-[[(3R)-1-[trans-4-hydroxy-4-(6-methoxy-3-pyridinyl)cyclohexyl]-3-pyrrolidinyl]amino]-2-oxoethyl]-3-(trifluoromethyl)-benzamide, dimethanesulfonate. CAS Number: 887401-93-6. Molecular Formula: C26H31F3N4O4 . 2CH3SO3H. Formula Weight: 712.8. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 11 mg/ml, DMSO: 12 mg/ml, PBS (pH 7.2): 5 mg/ml. lambdamax: 220, 274 nm. SMILES: O[C@]1(C2=CN=C(OC)C=C2)CC[C@@H](N3C[C@H](NC(CNC(C4=CC(C(F)(F)F)=CC=C4)=O)=O)CC3)CC1.CS(=O)(O)=O.CS(=O)(O)=O. InChi Code: InChI=1S/C26H31F3N4O4.2CH4O3S/c1-37-23-6-5-19(14-30-23)25(36)10-7-21(8-11-25)33-12-9-20(16-33)32-22(34)15-31-24(35)17-3-2-4-18(13-17)26(27,28)29,2*1-5(2,3)4/h2-6,13-14,20-21,36H,7-12,15-16H2,1H3,(H,31,35)(H,32,34),2*1H3,(H,2,3,4)/t20-,21-,25-,,/m1../. InChi Key: PNPNUHKICDECDH-FBLZNNLISA-N.