PF 429242 dihydrochloride

Name: PF 429242 dihydrochloride
Brand: Tocris Bioscience
SKU: 3354

Tocris Bioscience, part of Bio-Techne | Catalog # 3354

Citations (6)

COA / SDS

Competitive inhibitor of SREBP site 1 protease

Key Product Details

Description:	Competitive inhibitor of SREBP site 1 protease
Chemical Name:	4-[(Diethylamino)methyl]-N-[2-(2-methoxyphenyl)ethyl]-N-(3R)-3-pyrrolidinylbenzamide dihydrochloride
Purity:	≥97% (HPLC)
Molecular Weight:	482.49

View Full Technical Details for PF 429242 dihydrochloride

Technical Data
Citations

Biological Activity for PF 429242 dihydrochloride

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.

Compound Libraries for PF 429242 dihydrochloride

PF 429242 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.

Technical Data for PF 429242 dihydrochloride

M. Wt	482.49
Formula	C₂₅H₃₅N₃O₂.2HCl
Storage	Desiccate at RT
Purity	≥97% (HPLC)
CAS Number	2248666-66-0
PubChem ID	90488837
InChi Key	GSUZWFZKTIOWTI-MQWQBNKOSA-N
Smiles	O=C(C2=CC=C(CN(CC)CC)C=C2)N(CCC3=CC=CC=C3OC)[C@@H]1CCNC1.Cl.Cl

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

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for PF 429242 dihydrochloride

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	water	24.12	50
	DMSO	24.12	50

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 will affect the solvent volumes required to prepare stock solutions.

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

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References for PF 429242 dihydrochloride

References are publications that support the biological activity of the 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