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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).

PF-04634817

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).
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
Targets&IC50
CCR5:470 nM, CCR2 (rat):20.8 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].
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 | Shipping with blue ice.
Solubility Information
DMSO: 50 mg/mL (97.74 mM), Sonication is recommended.
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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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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