PF-429242
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    WARNING: This product is for research use only, not for human or veterinary use.

Hodoodo CAT#: H525966

CAS#: 947303-87-9

Description: PF-429242 is a competitive inhibitor of sterol regulatory element-binding protein (SREBP) site 1 protease (IC50 = 0.175 μM). It is selective for site 1 protease against a panel of serine proteases. PF-429242 inhibits rate of cholesterol synthesis in CHO cells (IC50 = 0.53 μM).

Chemical Structure

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PF-429242
CAS# 947303-87-9
Instruction

Theoretical Analysis

Hodoodo Cat#: H525966
Name: PF-429242
CAS#: 947303-87-9
Chemical Formula: C25H35N3O2
Exact Mass: 409.27
Molecular Weight: 409.574
Elemental Analysis: C, 73.31; H, 8.61; N, 10.26; O, 7.81

Price and Availability

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1g USD -1 2 Weeks
2g USD -1 2 Weeks
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Synonym: PF-429242; PF 429242; PF429242.

IUPAC/Chemical Name: (R)-4-((diethylamino)methyl)-N-(2-methoxyphenethyl)-N-(pyrrolidin-3-yl)benzamide

InChi Key: XKPJTOHUPQWSOJ-HSZRJFAPSA-N

InChi Code: InChI=1S/C25H35N3O2/c1-4-27(5-2)19-20-10-12-22(13-11-20)25(29)28(23-14-16-26-18-23)17-15-21-8-6-7-9-24(21)30-3/h6-13,23,26H,4-5,14-19H2,1-3H3/t23-/m1/s1

SMILES Code: O=C(N(CCC1=CC=CC=C1OC)[C@H]2CNCC2)C3=CC=C(CN(CC)CC)C=C3

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 409.57 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.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Monnerie H, Romer M, Jensen BK, Millar JS, Jordan-Sciutto KL, Kim SF, Grinspan JB. Reduced sterol regulatory element-binding protein (SREBP) processing through site-1 protease (S1P) inhibition alters oligodendrocyte differentiation in vitro. J Neurochem. 2016 Jul 6. doi: 10.1111/jnc.13721. [Epub ahead of print] PubMed PMID: 27385127.

2: Gholkar AA, Cheung K, Williams KJ, Lo YC, Hamideh SA, Nnebe C, Khuu C, Bensinger SJ, Torres JZ. Fatostatin Inhibits Cancer Cell Proliferation by Affecting Mitotic Microtubule Spindle Assembly and Cell Division. J Biol Chem. 2016 Aug 12;291(33):17001-8. doi: 10.1074/jbc.C116.737346. Epub 2016 Jul 4. PubMed PMID: 27378817.

3: Wen AM, Le N, Zhou X, Steinmetz NF, Popkin DL. Tropism of CPMV to Professional Antigen Presenting Cells Enables a Platform to Eliminate Chronic Infections. ACS Biomater Sci Eng. 2015 Nov 9;1(11):1050-1054. Epub 2015 Oct 20. PubMed PMID: 27280157; PubMed Central PMCID: PMC4894745.

4: Uchida L, Urata S, Ulanday GE, Takamatsu Y, Yasuda J, Morita K, Hayasaka D. 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. PubMed PMID: 26875984; PubMed Central PMCID: PMC4776201.

5: Urata S, Weyer J, Storm N, Miyazaki Y, van Vuren PJ, Paweska JT, Yasuda J. Analysis of Assembly and Budding of Lujo Virus. J Virol. 2015 Dec 30;90(6):3257-61. doi: 10.1128/JVI.03198-15. PubMed PMID: 26719243; PubMed Central PMCID: PMC4810620.

6: Shimada S, Posadas-Herrera G, Aoki K, Morita K, Hayasaka D. Therapeutic effect of post-exposure treatment with antiserum on severe fever with thrombocytopenia syndrome (SFTS) in a mouse model of SFTS virus infection. Virology. 2015 Aug;482:19-27. doi: 10.1016/j.virol.2015.03.010. Epub 2015 Mar 26. PubMed PMID: 25817401.

7: Bitter A, Nüssler AK, Thasler WE, Klein K, Zanger UM, Schwab M, Burk O. Human sterol regulatory element-binding protein 1a contributes significantly to hepatic lipogenic gene expression. Cell Physiol Biochem. 2015;35(2):803-15. doi: 10.1159/000369739. Epub 2015 Jan 30. PubMed PMID: 25634759.

8: Blanchet M, Sureau C, Guévin C, Seidah NG, Labonté P. SKI-1/S1P inhibitor PF-429242 impairs the onset of HCV infection. Antiviral Res. 2015 Mar;115:94-104. doi: 10.1016/j.antiviral.2014.12.017. Epub 2015 Jan 5. PubMed PMID: 25573299.

9: Burri DJ, da Palma JR, Kunz S, Pasquato A. Envelope glycoprotein of arenaviruses. Viruses. 2012 Oct 17;4(10):2162-81. doi: 10.3390/v4102162. Review. PubMed PMID: 23202458; PubMed Central PMCID: PMC3497046.

10: Blanchet M, Seidah NG, Labonté P. SKI-1/S1P inhibition: a promising surrogate to statins to block hepatitis C virus replication. Antiviral Res. 2012 Aug;95(2):159-66. doi: 10.1016/j.antiviral.2012.05.006. Epub 2012 May 22. Review. PubMed PMID: 22626636.

11: Olmstead AD, Knecht W, Lazarov I, Dixit SB, Jean F. 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 Jan;8(1):e1002468. doi: 10.1371/journal.ppat.1002468. Epub 2012 Jan 5. PubMed PMID: 22241994; PubMed Central PMCID: PMC3252376.

12: Pasquato A, Rochat C, Burri DJ, Pasqual G, de la Torre JC, Kunz S. Evaluation of the anti-arenaviral activity of the subtilisin kexin isozyme-1/site-1 protease inhibitor PF-429242. Virology. 2012 Feb 5;423(1):14-22. doi: 10.1016/j.virol.2011.11.008. Epub 2011 Dec 10. PubMed PMID: 22154237; PubMed Central PMCID: PMC3285533.

13: Urata S, Yun N, Pasquato A, Paessler S, Kunz S, de la Torre JC. 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. doi: 10.1128/JVI.02019-10. Epub 2010 Nov 10. PubMed PMID: 21068251; PubMed Central PMCID: PMC3020022.

14: Hawkins JL, Robbins MD, Warren LC, Xia D, Petras SF, Valentine JJ, Varghese AH, Wang IK, Subashi TA, Shelly LD, Hay BA, Landschulz KT, Geoghegan KF, Harwood HJ Jr. 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. doi: 10.1124/jpet.108.139626. Epub 2008 Jun 24. PubMed PMID: 18577702.