PF-4136309

PF-4136309 is a chemokine (C-C motif) receptor 2 (CCR2) antagonist (IC50s = 5.2, 13, and 17 nM for the human, rat, and mouse receptors, respectively). It also inhibits the voltage-gated potassium channel subtype Kv11.1 by 35% when used at a concentration of 10 µM. PF-4136309 decreases isolated human monocyte chemotaxis induced by chemokine (C-C motif) ligand 2 (CCL2) with an IC50 value of 3.9 nM.Formal Name: N-[2-[(3S)-3-[[trans-4-hydroxy-4-[5-(2-pyrimidinyl)-2-pyridinyl]cyclohexyl]amino]-1-pyrrolidinyl]-2-oxoethyl]-3-(trifluoromethyl)-benzamide. CAS Number: 1341224-83-6. Synonyms: INCB 8761. Molecular Formula: C29H31F3N6O3. Formula Weight: 568.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 20 mg/ml, DMSO: 5 mg/ml, Ethanol: 20 mg/ml, Ethanol:PBS(pH 7.2) (1:5): 0.17 mg/ml. lambdamax: 250 nm. SMILES: O=C(CNC(C1=CC(C(F)(F)F)=CC=C1)=O)N2C[C@@H](N[C@]3([H])CC[C@@](C4=CC=C(C5=NC=CC=N5)C=N4)(O)CC3)CC2. InChi Code: InChI=1S/C29H31F3N6O3/c30-29(31,32)21-4-1-3-19(15-21)27(40)36-17-25(39)38-14-9-23(18-38)37-22-7-10-28(41,11-8-22)24-6-5-20(16-35-24)26-33-12-2-13-34-26/h1-6,12-13,15-16,22-23,37,41H,7-11,14,17-18H2,(H,36,40)/t22-,23-,28-/m0/s1. InChi Key: ZNSVOHSYDRPBGI-LXWOLXCRSA-N.