PF-4136309

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 Specifications

CAS Number

[1341224-83-6]

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.