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PF-04634817

Catalog No. T12419L CAS 1228111-63-4

PF-0463481 is safe and well-tolerated and has the potential for the study of diabetic nephropathy. PF-0463481 is an effective and orally active dual CCR2/CCR5 antagonist. It also has comparable human and rodent CCR2 potency (rat IC50=20.8 nM). PF-0463481 shows 10-20 fold less rodent CCR5 potency (rat IC50=470 nM).

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PF-04634817, CAS 1228111-63-4

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Purity: 98%

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Storage & Solubility Information

Description	PF-0463481 is safe and well-tolerated and has the potential for the study of diabetic nephropathy. PF-0463481 is an effective and orally active dual CCR2/CCR5 antagonist. It also has comparable human and rodent CCR2 potency (rat IC50=20.8 nM). PF-0463481 shows 10-20 fold less rodent CCR5 potency (rat IC50=470 nM).
Targets&IC50	Rat CCR2:20.8 nM, CCR5:470 nM
In vivo	PF-04634817 (p.o.; 30 mg/kg; once daily; 31 days intervention (weeks 2-15 after Streptozotocin)) intervention at the onset of diabetes (week 2) has no impact on the fasting blood glucose levels in diabetic Nos3-/- 221 mice. Early intervention with PF-04634817 induces an additional increase in glycated hemoglobin (HbA1c) levels. The development of diabetes causes a marked increase in the levels of glycated haemoglobin (HbA1c) in Nos3-/- mice [1].

Molecular Weight	511.58
Formula	C25H36F3N5O3
CAS No.	1228111-63-4

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 50 mg/mL (97.74 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. 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. 2. 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. 3. 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.

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Keywords

PF-04634817 1228111-63-4 免疫与炎症微生物学 CCR PF 04634817 PF04634817 Inhibitor inhibitor inhibit

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