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Tocris/PF 429242/3354/50/50 mg

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货号: 3354/50

品牌: Tocris

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Description: Competitive inhibitor of SREBP site 1 protease

Chemical Name: 4-[(Diethylamino)methyl]-N-[2-(2-methoxyphenyl)ethyl]-N-(3R)-3-pyrrolidinylbenzamide

Purity: ≥97% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

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

PF 429242 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	482.49
Formula	C₂₅H₃₅N₃O₂.2HCl
Storage	Desiccate at RT
Purity	≥97% (HPLC)
CAS Number	947303-87-9
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	24.12	50
	ethanol	48.25	100
	water	24.12	50

Preparing Stock Solutions

The following data is based on the product molecular weight 482.49. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.07 mL	10.36 mL	20.73 mL
5 mM	0.41 mL	2.07 mL	4.15 mL
10 mM	0.21 mL	1.04 mL	2.07 mL
50 mM	0.04 mL	0.21 mL	0.41 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Hay et al (2007) Aminopyrrolidineamide inhibitors of site-1 protease. Bioorg.Med.Chem.Lett. 17 4411 PMID: 17583500

Hawkins et al (2008) 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. 326 801 PMID: 18577702

Urata et al (2011) Antiviral activity of a small-molecule inhibitor of arenavirus glycoprotein processing by the cellular site 1 protease. J.Virol. 85 795 PMID: 21068251

Olmstead (2012) 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. 8 e1002468 PMID: 22241994

Keywords: PF 429242, supplier, SREBP, sterol, regulatory, element, binding, proteins, inhibitors, inhibits, site, 1, proteases, S1P, serine, antivirals, PF429242, Other, Proteases, Antivirals, SREBP, SREBP, Tocris Bioscience

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