PF 429242 dihydrochloride

Key Product Details

Product Description

PF 429242 dihydrochloride is a reversible, competitive inhibitor of sterol regulatory element-binding protein (SREBP) site 1 protease (IC₅₀ = 0.175 μM). Selective for site 1 protease against a panel of serine proteases. Inhibits rate of cholesterol synthesis in CHO cells (IC₅₀ = 0.53 μM). Also displays antiviral activity. Cell permeable.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Product Specifications for PF 429242 dihydrochloride

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for PF 429242 dihydrochloride

The following data is based on the product molecular weight 482.49.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.5 mM	4.15 mL	20.73 mL	41.45 mL
2.5 mM	0.83 mL	4.15 mL	8.29 mL
5 mM	0.41 mL	2.07 mL	4.15 mL
25 mM	0.08 mL	0.41 mL	0.83 mL

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 7 publications citing the usage of this product.

• Olmstead Human subtilase SKI-1/S1P is a master regulator of the HCV lifecycle and a potential host cell target for developing indirect-acting antiviral agents. PLoS.Pathog. 2012 PMID: 22241994
• Hawkins 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 PMID: 18577702
• Urata Antiviral activity of a small-molecule inhibitor of arenavirus glycoprotein processing by the cellular site 1 protease. J.Virol. 2011 PMID: 21068251
• Hay Aminopyrrolidineamide inhibitors of site-1 protease. Bioorg.Med.Chem.Lett. 2007 PMID: 17583500

Product Documents for PF 429242 dihydrochloride