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PF 429242 S1P Receptor inhibitor

Name: PF 429242
Brand: Selleck Chemicals
SKU: S6418
Availability: InStock
Rating: 5 (2 reviews)

Cat.No.S6418

PF 429242 is known as a S1P inhibitor with an IC50 of 170 nM, showing no significant inhibition of trypsin, elastase, proteinase K, plasmin, kallikren, factor XIa, thrombin, or furin at concentrations up to 100 μM and only modest inhibition of urokinase (IC50 = 50 μM) and factor Xa (IC50 = 100 μM).

Chemical Structure

Molecular Weight: 409.56

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 98.99%

98.99

Related Targets	Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras GPR GluR Prostaglandin Receptor CXCR Adenosine Receptor P2 Receptor CCR Angiotensin Receptor Hedgehog/Smoothened PKA Cannabinoid Receptor cAMP Glucagon Receptor SGLT Opioid Receptor Sigma Receptor PAR Endothelin Receptor LTR Neurokinin Receptor Guanylate Cyclase PKG LPA Receptor OX Receptor
Related Products	JTE 013 SEW 2871 Etrasimod(APD334) MP-A08 SLF1081851 hydrochloride K145 CAY10444 CYM5541 Sphingosine-1-phosphate CYM-5520 CYM50308 W146

Chemical Information, Storage & Stability

Molecular Weight	409.56	Formula	C₂₅H₃₅N₃O₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	947303-87-9	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CCN(CC)CC1=CC=C(C=C1)C(=O)N(CCC2=CC=CC=C2OC)C3CCNC3

Solubility

In vitro
Batch:

DMSO : 82 mg/mL (200.21 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 82 mg/mL

Ethanol : 82 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.100mg/ml (10.01mM)	Taking the 1 mL working solution as an example, add 50 μL of 82 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.510mg/ml (1.25mM)	Taking the 1 mL working solution as an example, add 50 μL of 10.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	S1P ^[1] (Cell-free assay) 170 nM
In vitro	In cultured human liver (Hep-G2) cells, PF-429242 prevents proteolytic processing and nuclear translocation of SREBP, reduces the expression of key genes involved in cholesterol synthesis and fatty acid synthesis, and inhibits both pathways in the absence of any cytotoxicity^[1]. The addition of PF-429242 suppresses the viral propagation of all serotypes of DENV in several primate-derived cells^[2].
In vivo	PK data for PF-429242 show that it had rapid clearance (CL = 75 ml/min/kg) and poor oral bioavailability (5%) in rats^[1].
References	[1] https://pubmed.ncbi.nlm.nih.gov/17583500/ [2] https://pubmed.ncbi.nlm.nih.gov/26875984/

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