PF-4634817

Product Name: PF-4634817
CAS No.: 1228111-63-4
Chemical Name: PF-4634817
Synonyms: PF-4634817;PF-04634817;PF 04634817,PF04634817;D-erythro-Pentitol, 1,5-anhydro-2,3-dideoxy-4-O-methyl-3-[[(1R,3S)-3-(1-methylethyl)-3-[[(1S,4S)-5-[6-(trifluoromethyl)-4-pyrimidinyl]-2,5-diazabicyclo[2.2.1]hept-2-yl]carbonyl]cyclopentyl]amino]-
CBNumber: CB13160418
Molecular Formula: C25H36F3N5O3
Formula Weight: 511.58
MOL File: 1228111-63-4.mol

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PF-4634817 Property

Boiling point:: 630.3±55.0 °C(Predicted)
Density: 1.30±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMSO: 50 mg/mL (97.74 mM)
form: Solid
pka: 8.62±0.40(Predicted)
color: White to off-white

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: PZ0309
Product name: PF-04634817 succinate
Purity: ≥98%(HPLC)
Packaging: 25mg
Price: $463
Updated: 2025/07/31

ChemScene

Product number: CS-0066648
Product name: PF-04634817
Purity: 98.87%
Packaging: 1mg
Price: $190
Updated: 2021/12/16

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PF-4634817 Chemical Properties,Usage,Production

Uses

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].

in vivo

PF-04634817 (oral administration; 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. The development of diabetes results in a marked increase in the levels of glycated haemoglobin (HbA1c) in Nos3^-/- mice. Early intervention with PF-04634817 induces an additional increase in glycated hemoglobin (HbA1c) levels^[1].

Animal Model:	Nos3^-/- mice on the C57BL/6 background^[1]
Dosage:	30 mg/kg
Administration:	Oral administration; once daily; 31 days intervention (weeks 2-15 after Streptozotocin)
Result:	Had no impact on the fasting blood glucose levels, but induced an additional increase in HbA1c levels.

IC 50

Rat CCR2: 20.8 nM (IC₅₀); CCR5: 470 nM (IC₅₀)

References

[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. DOI:10.1152/ajprenal.00340.2019
[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. DOI:10.1167/iovs.17-22731
[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. DOI:10.1016/j.ekir.2018.07.010

PF-4634817 Preparation Products And Raw materials

Raw materials

Preparation Products

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PF-4634817 Suppliers

China 13 United States 4 Global 17

ShangHai Caerulum Pharma Discovery Co., Ltd.

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TargetMol Chemicals Inc.

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Email: marketing@targetmol.com
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https://hanhongsci.com/

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1228111-63-4, PF-4634817Related Search:

PF-05231023 PF 05175157 PF-04691502

PF-04634817

PF-4634817

D-erythro-Pentitol, 1,5-anhydro-2,3-dideoxy-4-O-methyl-3-[[(1R,3S)-3-(1-methylethyl)-3-[[(1S,4S)-5-[6-(trifluoromethyl)-4-pyrimidinyl]-2,5-diazabicyclo[2.2.1]hept-2-yl]carbonyl]cyclopentyl]amino]-

PF 04634817,PF04634817

1228111-63-4

C25H36F3N5O3