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PF-04634817

PF-04634817
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PF-04634817

Catalog No. T12419LCas No. 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).
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
25 mg$1,8208-10 weeks
50 mg$2,3808-10 weeks
100 mg$3,1008-10 weeks
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Product Introduction

Bioactivity
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
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].
Chemical Properties
Molecular Weight511.58
FormulaC25H36F3N5O3
Cas No.1228111-63-4
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 50 mg/mL (97.74 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.9547 mL9.7736 mL19.5473 mL97.7364 mL
5 mM0.3909 mL1.9547 mL3.9095 mL19.5473 mL
10 mM0.1955 mL0.9774 mL1.9547 mL9.7736 mL
20 mM0.0977 mL0.4887 mL0.9774 mL4.8868 mL
50 mM0.0391 mL0.1955 mL0.3909 mL1.9547 mL

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