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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

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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
Smiles	C(=O)([C@]1([C@@H](C)C)C[C@H](N[C@@H]2[C@H](OC)COCC2)CC1)N3[C@@]4(CN([C@](C3)(C4)[H])C=5C=C(C(F)(F)F)N=CN5)[H]
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 recommended.

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 stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

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