PF-4136309

• CAT Number: I001304
• CAS Number: 1341224-83-6
• Molecular Formula: C29H31F3N6O3
• Molecular Weight: 568.6
• Purity: ≥95%
• Target: CCR2
• Solubility: DMSO: ≥ 32 mg/mL
• Storage: -20°C
• IUPAC Name: N-[2-[(3S)-3-[[4-hydroxy-4-(5-pyrimidin-2-ylpyridin-2-yl)cyclohexyl]amino]pyrrolidin-1-yl]-2-oxoethyl]-3-(trifluoromethyl)benzamide
• InChI: 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
• InChIKey: ZNSVOHSYDRPBGI-CBQRAPNFSA-N
• SMILES: C1CC(CCC1NC2CCN(C2)C(=O)CNC(=O)C3=CC(=CC=C3)C(F)(F)F)(C4=NC=C(C=C4)C5=NC=CC=N5)O

PF-4136309 (Cat No.: I001304) is a potent and selective antagonist of CCR2, a chemokine receptor involved in inflammation and immune responses. It effectively inhibits CCR2 in humans, mice, and rats with impressive IC50 values of 5.2 nM, 17 nM, and 13 nM, respectively. This selectivity and potency make PF-4136309 a valuable tool for researchers studying chemokine receptor biology and exploring potential therapeutic interventions targeting CCR2-mediated pathways. If you need to, please contact us in time, and we will reply to you as soon as possible within 24 hours.

Reference

1:ACS Med Chem Lett. 2011 Oct 5;2(12):913-8. doi: 10.1021/ml200199c. eCollection 2011 Dec 8. Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist.Xue CB,Wang A,Han Q,Zhang Y,Cao G,Feng H,Huang T,Zheng C,Xia M,Zhang K,Kong L,Glenn J,Anand R,Meloni D,Robinson DJ,Shao L,Storace L,Li M,Hughes RO,Devraj R,Morton PA,Rogier DJ,Covington M,Scherle P,Diamond S,Emm T,Yeleswaram S,Contel N,Vaddi K,Newton R,Hollis G,Metcalf B, PMID: 24900280 PMCID: PMC4018168 DOI: 10.1021/ml200199c Abstract: We report the discovery of a new (S)-3-aminopyrrolidine series of CCR2 antagonists. Structure-activity relationship studies on this new series led to the identification of 17 (INCB8761/PF-4136309) that exhibited potent CCR2 antagonistic activity, high selectivity, weak hERG activity, and an excellent in vitro and in vivo ADMET profile. INCB8761/PF-4136309 has entered human clinical trials.