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PF-543 Citrate

Name: PF-543 Citrate
Brand: TargetMol
SKU: T12436
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T12436Cas No. 1415562-83-2

Alias Sphingosine Kinase 1 Inhibitor II Citrate, PF543 Citrate

PF-543 Citrate (Sphingosine Kinase 1 Inhibitor II Citrate) is a selective and potent inhibitor of sphingosine kinase 1 (SPHK1) and is an efficient inhibitor of 1-phosphate sphingosine (S1P) formation. It possesses anticancer, antifibrotic, and anti-inflammatory activities and can be used in research on colorectal cancer.

PF-543 Citrate

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Purity: 99.33%

Catalog No. T12436Alias Sphingosine Kinase 1 Inhibitor II Citrate, PF543 CitrateCas No. 1415562-83-2

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
1 mg	$30	-	In Stock

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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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Batch Information

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Purity:99.33%

Appearance:Solid

Color:White

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COA

Product Introduction

Bioactivity

Description	PF-543 Citrate (Sphingosine Kinase 1 Inhibitor II Citrate) is a selective and potent inhibitor of sphingosine kinase 1 (SPHK1) and is an efficient inhibitor of 1-phosphate sphingosine (S1P) formation. It possesses anticancer, antifibrotic, and anti-inflammatory activities and can be used in research on colorectal cancer.
Targets&IC50	S1P:26.7 nM, SPHK1:3.6 nM (Ki), SPHK1:2 nM
In vitro	PF-543 Citrate is a selective sphingosine competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 Citrate is also a potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 Citrate inhibits the formation of C17-S1P in 1483 cells with IC50 of 1.0 nM. [1]
In vivo	Administration of PF-543 Citrate (1 mg/kg intrperitoneal injection every other day for 21 days) in a mouse hypoxic model of pulmonary hypertension had no effect on vascular remodeling but reduced right ventricular hypertrophy. PF-543 Citrate (10 mg/kg or 30 mg/kg intraperitoneally, 24h), T1/2 in mouse blood samples was 1.2 h. Administration of 10 mg/kg PF-543 Citrate to mice for 24 hours induced a decrease in SK1 expression in pulmonary vessels. [2] The inhibition of SPHK1 and S1PR2 activity by PF-543 Citrate significantly hindered pancreatic fibrosis in CP mice. [4]
Synonyms	Sphingosine Kinase 1 Inhibitor II Citrate, PF543 Citrate

Chemical Properties

Molecular Weight	657.73
Formula	C₃₃H₃₉NO₁₁S
Cas No.	1415562-83-2
Smiles	C(CC(O)=O)(CC(O)=O)(C(O)=O)O.C(N1[C@@H](CO)CCC1)C2=CC=C(COC3=CC(CS(=O)(=O)C4=CC=CC=C4)=CC(C)=C3)C=C2
Relative Density.	no data available

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

H2O: 40 mg/mL (60.82 mM), Sonication is recommended.

DMSO: 80 mg/mL (121.63 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (5.02 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

H2O/DMSO

	1mg	5mg	10mg	50mg
1 mM	1.5204 mL	7.6019 mL	15.2038 mL	76.0190 mL
5 mM	0.3041 mL	1.5204 mL	3.0408 mL	15.2038 mL
10 mM	0.1520 mL	0.7602 mL	1.5204 mL	7.6019 mL
20 mM	0.0760 mL	0.3801 mL	0.7602 mL	3.8010 mL
50 mM	0.0304 mL	0.1520 mL	0.3041 mL	1.5204 mL

DMSO

	1mg	5mg	10mg	50mg
100 mM	0.0152 mL	0.0760 mL	0.1520 mL	0.7602 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