PF-4136309

• Description :

  PF-4136309 is a potent, selective, and orally bioavailable CCR2 antagonist, with IC50s of 5.2 nM, 17 nM and 13 nM for human, mouse and rat CCR2.

• Product Name Alternative :

  INCB8761

• UNSPSC :

  12352005

• Hazard Statement :

  H302, H315, H319, H335

• Target :

  CCR

• Type :

  Reference compound

• Related Pathways :

  GPCR/G Protein; Immunology/Inflammation

• Applications :

  COVID-19-immunoregulation

• Field of Research :

  Inflammation/Immunology; Endocrinology

• Assay Protocol :

  https://www.medchemexpress.com/PF-4136309.html

• Purity :

  99.86

• Solubility :

  DMSO : ≥ 34 mg/mL|Ethanol : 133.33 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL (ultrasonic; warming; heat to 60°C)

• Smiles :

  O[C@]1(CC[C@](CC1)([H])N[C@@H]2CN(CC2)C(CNC(C3=CC=CC(C(F)(F)F)=C3)=O)=O)C4=NC=C(C=C4)C5=NC=CC=N5

• Molecular Formula :

  C29H31F3N6O3

• Molecular Weight :

  568.59

• Precautions :

  H302, H315, H319, H335

• References & Citations :

  [1]Xue CB, et al. Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist. ACS Med. Chem. Lett., 2011, 2 (12), pp 913-918.|[2]Wang W, Chen XK, Zhou L, et al. Chemokine CCL2 promotes cardiac regeneration and repair in myocardial infarction mice via activation of the JNK/STAT3 axis. Acta Pharmacol Sin. Published online December 12, 2023.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Phase 2

• Isoform :

  CCR2

• CAS Number :

  [1341224-83-6]