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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).

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Pack Size	Price	Availability
25 mg	$1,820	8-10 weeks
50 mg	$2,380	8-10 weeks
100 mg	$3,100	8-10 weeks

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Product Introduction

Bioactivity

Description

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 Weight	511.58
Formula	C25H36F3N5O3
Cas No.	1228111-63-4

Storage & Solubility Information

Storage

Powder: -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

	1mg	5mg	10mg	50mg
1 mM	1.9547 mL	9.7736 mL	19.5473 mL	97.7364 mL
5 mM	0.3909 mL	1.9547 mL	3.9095 mL	19.5473 mL
10 mM	0.1955 mL	0.9774 mL	1.9547 mL	9.7736 mL
20 mM	0.0977 mL	0.4887 mL	0.9774 mL	4.8868 mL
50 mM	0.0391 mL	0.1955 mL	0.3909 mL	1.9547 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

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A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

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