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PF429242 dihydrochloride

Catalog No. T12437   CAS 2248666-66-0

PF429242 dihydrochloride can reversibly inhibit S1P (IC50 of 175 nM).

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PF429242 dihydrochloride Chemical Structure
PF429242 dihydrochloride, CAS 2248666-66-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 36.00
2 mg In stock $ 52.00
5 mg In stock $ 85.00
10 mg In stock $ 148.00
25 mg In stock $ 297.00
50 mg In stock $ 545.00
100 mg In stock $ 785.00
1 mL * 10 mM (in DMSO) In stock $ 94.00
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Purity: 98.67%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PF429242 dihydrochloride can reversibly inhibit S1P (IC50 of 175 nM).
Targets&IC50 S1P:175 nM
In vitro 10 μM PF-429242 down-regulates the signal from an SRE-luciferase reporter gene in human embryonic kidney 293 cells and the expression of endogenous SREBP target genes in cultured HepG2 cells. In HepG2 cells, PF-429242 inhibits cholesterol synthesis, with an IC50 of 0.5 μM[1]. PF-429242 treatment also shows suppressive effects on DENV2 yields in the cultured fluids of human-derived HEK-293, Hep G2, and non-human-primate derived LLC-MK2 cells[2]. PF-429242 has potent antiviral against LCMV and LASV [3].
In vivo PF-429242 inhibits the expression of hepatic SREBP target genes, and the hepatic rates of cholesterol and fatty acid synthesis are reduced In mice[1].
Molecular Weight 482.49
Formula C25H37Cl2N3O2
CAS No. 2248666-66-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 50 mg/mL (103.63 mM), Sonification is recommended.

DMSO: 83.3 mg/mL (165.81 mM)

TargetMolReferences and Literature

1. Hawkins JL, et al. Pharmacologic inhibition of site 1 protease activity inhibits sterol regulatory element-binding protein processing and reduces lipogenic enzyme gene expression and lipid synthesis in cultured cells and experimental animals. J Pharmacol Exp Ther. 2008 Sep;326(3):801-8. 2. Uchida L, et al. Suppressive Effects of the Site 1 Protease (S1P) Inhibitor, PF-429242, on Dengue Virus Propagation. Viruses. 2016 Feb 10;8(2). pii: E46. doi: 10.3390/v8020046. 3. Urata S, et al. Antiviral activity of a small-molecule inhibitor of arenavirus glycoprotein processing by the cellular site 1 protease. J Virol. 2011 Jan;85(2):795-803.

Related compound libraries

This product is contained In the following compound libraries:
GPCR Compound Library Inhibitor Library NO PAINS Compound Library Anti-Infection Compound Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

PF429242 dihydrochloride 2248666-66-0 GPCR/G Protein S1P Receptor PF429242 PF-429242 Dihydrochloride PF-429242 dihydrochloride Virus Protease inhibit Inhibitor PF 429242 Dihydrochloride PF-429242 Fatty Acid Synthase (FASN) PF 429242 PF429242 Dihydrochloride inhibitor

 

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