PF-04634817

PF-0463481 is a potent and orally active dual CCR2/CCR5 antagonist with comparable human and rodent CCR2 potency (rat IC50=20.8 nM), and displays 10-20 fold less rodent CCR5 potency (rat IC50=470 nM) . PF-0463481 is safe and well-tolerated and has the potential for the study of diabetic nephropathy[3].

Product Specifications

CAS Number

[1228111-63-4]

UNSPSC

12352005

Target

CCR

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation

Applications

Neuroscience-Neuromodulation

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/pf-04634817.html

Purity

98.87

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

O=C(N1[C@@]2([H])C[C@@]([H])(C1)N(C3=NC=NC(C(F)(F)F)=C3)C2)[C@@]4(C[C@@H](CC4)N[C@@H]5[C@@H](COCC5)OC)C(C)C

Molecular Formula

C25H36F3N5O3

Molecular Weight

511.58

References & Citations

[1]Gale JD, et al. A CCR2/5 Inhibitor, PF-04634817, Is Inferior to Monthly Ranibizumab in the Treatment of Diabetic Macular Edema. Invest Ophthalmol Vis Sci. 2018 May 1;59 (6) :2659-2669.|[2]Gale JD, et al. Effect of PF-04634817, an Oral CCR2/5 Chemokine Receptor Antagonist, on Albuminuria in Adults with Overt Diabetic Nephropathy. Kidney Int Rep. 2018 Aug 3;3 (6) :1316-1327.|[3]Tesch GH, et al. Combined inhibition of CCR2 and ACE provides added protection against progression of diabetic nephropathy in Nos3-deficient mice.Am J Physiol Renal Physiol. 2019 Dec 1;317 (6) :F1439-F1449.