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PF-04634817

Name: PF-04634817
Brand: TargetMol
SKU: T12419L
Rating: 4.5 (1 reviews)

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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

😃Good

Catalog No. T12419LCas No. 1228111-63-4

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

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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.

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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 shows 10-20 fold less rodent CCR5 potency (rat IC50=470 nM).
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 Weight	511.58
Formula	C₂₅H₃₆F₃N₅O₃
Cas No.	1228111-63-4
Relative Density.	1.30 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 50 mg/mL (97.74 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2.5 mg/mL (4.89 mM), Sonication is recommeded.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

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:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

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

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/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 μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc