PF 429242 dihydrochloride

Cat. No. 3354 6 篇引用文献提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Competitive inhibitor of SREBP site 1 protease

化学名： 4-[(Diethylamino)methyl]-N-[2-(2-methoxyphenyl)ethyl]-N-(3R)-3-pyrrolidinylbenzamide dihydrochloride

纯度： ≥97% (HPLC)

引用文献 (6)

文献 (1)

通路 (1)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 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.

许可信息

Sold for research purposes under agreement from Pfizer Inc.

化合物库 for PF 429242 dihydrochloride

PF 429242 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。

技术数据 for PF 429242 dihydrochloride

分子量	482.49
公式	C₂₅H₃₅N₃O₂.2HCl
储存	Desiccate at RT
纯度	≥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

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

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

溶解性数据 for PF 429242 dihydrochloride

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
	water	24.12	50
	DMSO	24.12	50

制备储备液 for PF 429242 dihydrochloride

以下数据基于产品分子量 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.

浓度/溶剂体积/质量	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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产品说明书 for PF 429242 dihydrochloride

分析证书/产品说明书

化学品安全技术说明书

参考文献 for PF 429242 dihydrochloride

参考文献是支持产品生物活性的出版物。

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

If you know of a relevant reference for PF 429242 dihydrochloride, please let us know.

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关键词: PF 429242 dihydrochloride, PF 429242 dihydrochloride supplier, SREBP, sterol, regulatory, element, binding, proteins, inhibitors, inhibits, site, 1, proteases, S1P, serine, antivirals, PF429242, Other, Proteases, Non-selective, Antivirals, 3354, Tocris Bioscience

6 篇 PF 429242 dihydrochloride 的引用文献

引用文献是使用了 Tocris 产品的出版物。 PF 429242 dihydrochloride 的部分引用包括：

Tien et al (2019) Ambient particulate matter attenuates Sirtuin1 and augments SREBP1-PIR axis to induce human pulmonary fibroblast inflammation: molecular mechanism of microenvironment associated with COPD. Aging (Albany NY) 11 4654 PMID: 31299012

Flint et al (2019) A genome-wide CRISPR screen identifies N-acetylglucosamine-1-phosphate transferase as a potential antiviral target for Ebola virus. Nat Commun 10 285 PMID: 30655525

Uchida et al (2016) Suppressive effects of the site 1 protease (S1P) inhibitor, PF-429242, on dengue virus propagation. Viruses 8 E46 PMID: 26875984

Kleinfelter et al (2015) Haploid Genetic Screen Reveals a Profound and Direct Dependence on Cholesterol for Hantavirus Membrane Fusion. Ann Rheum Dis 6 e00801 PMID: 26126854

Scott et al (2018) TFAP2 transcription factors are regulators of lipid droplet biogenesis. Elife 7 PMID: 30256193

Urata et al (2015) Analysis of Assembly and Budding of Lujo Virus. J Virol 90 3257 PMID: 26719243

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