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MedKoo Cat#: 525966 | Name: PF-429242

Description:

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

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

PF-429242
PF-429242
CAS#947303-87-9

Theoretical Analysis

MedKoo Cat#: 525966

Name: PF-429242

CAS#: 947303-87-9

Chemical Formula: C25H35N3O2

Exact Mass: 409.2729

Molecular Weight: 409.57

Elemental Analysis: C, 73.31; H, 8.61; N, 10.26; O, 7.81

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
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
Product Data
Product Data
Instruction
View handling instruction
Biological target:
PF 429242 is known as a S1P inhibitor with an IC50 of 170 nM.
In vitro activity:
This study evaluated the action of PF-429242 in human bronchial cells expressing the most frequent mutation of CFTR (p.Phe508del) found in patients. This study observed that PF-429242 increases the synthesis of the mRNA and the protein encoded by the CFTR gene harbouring the mutation. This study also observed that PF-429242 alleviates the defects of the p.Phe508del-CFTR channel in human Cystic Fibrosis cells. Reference: Bioorg Med Chem Lett. 2022 Sep 15;72:128866. https://pubmed.ncbi.nlm.nih.gov/35752380/
In vivo activity:
The volumes of RCC1 xenografts with PF-429242 administration were significantly lower than those with vehicle treatment (Fig. 5A). RCC1 xenograft growth was potently inhibited following PF-429242 injection (Fig. 5B). RCC1 xenografts with PF-429242 administration were significantly lighter than the vehicle-treated tumors (Fig. .5C). Mice body weights were not significantly different between the two groups (Fig. 5D), indicating that mice were well-tolerated to the PF-429242 treatment. Reference: Cell Death Dis. 2021 Jul 20;12(8):717. https://pubmed.ncbi.nlm.nih.gov/34285190/
Solvent mg/mL mM comments
Solubility
DMSO 82.0 200.21
Ethanol 82.0 200.21
Water 82.0 200.21
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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:
1. Huguet F, Guellec J, Kerbiriou M, Gandy M, Thomas J, Férec C, Benz N, Trouvé P. Evaluation of aminopyrrolidine amide to improve chloride transport in CFTR-defective cells. Bioorg Med Chem Lett. 2022 Sep 15;72:128866. doi: 10.1016/j.bmcl.2022.128866. Epub 2022 Jun 23. PMID: 35752380. 2. Gomes PS, Carneiro MPD, Machado PA, de Andrade-Neto VV, da Fonseca-Martins AM, Goundry A, Pereira da Silva JVM, Gomes DCO, Lima APCA, Ennes-Vidal V, Sodero ACR, De-Simone SG, de Matos Guedes HL. Subtilisin of Leishmania amazonensis as Potential Druggable Target: Subcellular Localization, In Vitro Leishmanicidal Activity and Molecular Docking of PF-429242, a Subtilisin Inhibitor. Curr Issues Mol Biol. 2022 May 9;44(5):2089-2106. doi: 10.3390/cimb44050141. PMID: 35678670; PMCID: PMC9164065. 3. Wang TB, Geng M, Jin H, Tang AG, Sun H, Zhou LZ, Chen BH, Shen G, Sun Q. SREBP1 site 1 protease inhibitor PF-429242 suppresses renal cell carcinoma cell growth. Cell Death Dis. 2021 Jul 20;12(8):717. doi: 10.1038/s41419-021-03999-9. PMID: 34285190; PMCID: PMC8292369.
In vitro protocol:
1. Huguet F, Guellec J, Kerbiriou M, Gandy M, Thomas J, Férec C, Benz N, Trouvé P. Evaluation of aminopyrrolidine amide to improve chloride transport in CFTR-defective cells. Bioorg Med Chem Lett. 2022 Sep 15;72:128866. doi: 10.1016/j.bmcl.2022.128866. Epub 2022 Jun 23. PMID: 35752380. 2. Gomes PS, Carneiro MPD, Machado PA, de Andrade-Neto VV, da Fonseca-Martins AM, Goundry A, Pereira da Silva JVM, Gomes DCO, Lima APCA, Ennes-Vidal V, Sodero ACR, De-Simone SG, de Matos Guedes HL. Subtilisin of Leishmania amazonensis as Potential Druggable Target: Subcellular Localization, In Vitro Leishmanicidal Activity and Molecular Docking of PF-429242, a Subtilisin Inhibitor. Curr Issues Mol Biol. 2022 May 9;44(5):2089-2106. doi: 10.3390/cimb44050141. PMID: 35678670; PMCID: PMC9164065.
In vivo protocol:
1. Wang TB, Geng M, Jin H, Tang AG, Sun H, Zhou LZ, Chen BH, Shen G, Sun Q. SREBP1 site 1 protease inhibitor PF-429242 suppresses renal cell carcinoma cell growth. Cell Death Dis. 2021 Jul 20;12(8):717. doi: 10.1038/s41419-021-03999-9. PMID: 34285190; PMCID: PMC8292369.
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.