MedKoo Cat#: 465006 | Name: Pefabloc

Description:

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

Pefabloc is an irreversible serine proteinase inhibitor. Pefabloc efficiently inhibits both human and rat platelet activating factor (PAF)-degrading acetylhydrolase (acetylhydrolase).

Chemical Structure

Pefabloc
Pefabloc
CAS#2131171-67-8

Theoretical Analysis

MedKoo Cat#: 465006

Name: Pefabloc

CAS#: 2131171-67-8

Chemical Formula: C31H33N5O4S2

Exact Mass: 603.1974

Molecular Weight: 603.76

Elemental Analysis: C, 61.67; H, 5.51; N, 11.60; O, 10.60; S, 10.62

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 #
2131171-67-8;
Synonym
Pefabloc; Pefabloc PL
IUPAC/Chemical Name
1-((S)-3-(3-carbamimidoylphenyl)-2-(naphthalene-2-sulfonamido)propanoyl)-N-(thiophen-2-ylmethyl)piperidine-3-carboxamide
InChi Key
PIFQUSTVOQWPJQ-NMXAJACMSA-N
InChi Code
InChI=1S/C31H33N5O4S2/c32-29(33)24-9-3-6-21(16-24)17-28(35-42(39,40)27-13-12-22-7-1-2-8-23(22)18-27)31(38)36-14-4-10-25(20-36)30(37)34-19-26-11-5-15-41-26/h1-3,5-9,11-13,15-16,18,25,28,35H,4,10,14,17,19-20H2,(H3,32,33)(H,34,37)/t25?,28-/m0/s1
SMILES Code
O=C(N1CCCC(C(NCC2=CC=CS2)=O)C1)[C@H](CC3=CC(C(N)=N)=CC=C3)NS(C4=CC5=CC=CC=C5C=C4)(=O)=O
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
>3 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

Preparing Stock Solutions

The following data is based on the product molecular weight 603.76 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
1: Patrick ME, Egland KA. SUSD2 Proteolytic Cleavage Requires the GDPH Sequence and Inter-Fragment Disulfide Bonds for Surface Presentation of Galectin-1 on Breast Cancer Cells. Int J Mol Sci. 2019 Aug 5;20(15). pii: E3814. doi: 10.3390/ijms20153814. PubMed PMID: 31387209; PubMed Central PMCID: PMC6696261. 2: Cai CX, Schneck NA, Zhao W, Blackstock D, Cai J, Harris D, Ivleva VB, Gollapudi D, Horwitz J, Arnold FJ, Cooper JW, Lei QP. Characterization of AEBSF-antibody modifications for a protease inhibitor supplementation strategy. Anal Bioanal Chem. 2019 Sep;411(23):6111-6118. doi: 10.1007/s00216-019-01995-9. Epub 2019 Aug 1. PubMed PMID: 31367804. 3: Poonsin T, Simpson BK, Benjakul S, Visessanguan W, Yoshida A, Osatomi K, Klomklao S. Anionic trypsin from the spleen of albacore tuna (Thunnus alalunga): Purification, biochemical properties and its application for proteolytic degradation of fish muscle. Int J Biol Macromol. 2019 Jul 15;133:971-979. doi: 10.1016/j.ijbiomac.2019.04.122. Epub 2019 Apr 24. PubMed PMID: 31028808. 4: Cai CX, Schneck NA, Harris D, Blackstock D, Ivleva VB, Cheng KC, Charlton A, Arnold FJ, Cooper JW, Lei QP. Quantification of residual AEBSF-related impurities by reversed-phase liquid chromatography. J Chromatogr B Analyt Technol Biomed Life Sci. 2019 May 15;1116:19-23. doi: 10.1016/j.jchromb.2019.03.022. Epub 2019 Mar 20. PubMed PMID: 30953918. 5: Prezoto BC, Kato EE, Gonçalves LRC, Sampaio SC, Sano-Martins IS. Elevated plasma levels of hepatocyte growth factor in rats experimentally envenomated with Bothrops jararaca venom: Role of snake venom metalloproteases. Toxicon. 2019 Apr 15;162:9-14. doi: 10.1016/j.toxicon.2019.03.003. Epub 2019 Mar 6. PubMed PMID: 30849454. 6: Hill ME, Yildiz M, Hardy JA. Cysteine Disulfide Traps Reveal Distinct Conformational Ensembles in Dengue Virus NS2B-NS3 Protease. Biochemistry. 2019 Feb 12;58(6):776-787. doi: 10.1021/acs.biochem.8b00978. Epub 2018 Dec 17. PubMed PMID: 30472839. 7: Flores-Fernández CN, Cárdenas-Fernández M, Dobrijevic D, Jurlewicz K, Zavaleta AI, Ward JM, Lye GJ. Novel extremophilic proteases from Pseudomonas aeruginosa M211 and their application in the hydrolysis of dried distiller's grain with solubles. Biotechnol Prog. 2019 Jan;35(1):e2728. doi: 10.1002/btpr.2728. Epub 2018 Oct 22. PubMed PMID: 30304581. 8: Yoon H, Schaubeck M, Lagkouvardos I, Blesl A, Heinzlmeir S, Hahne H, Clavel T, Panda S, Ludwig C, Kuster B, Manichanh C, Kump P, Haller D, Hörmannsperger G. Increased Pancreatic Protease Activity in Response to Antibiotics Impairs Gut Barrier and Triggers Colitis. Cell Mol Gastroenterol Hepatol. 2018 May 29;6(3):370-388.e3. doi: 10.1016/j.jcmgh.2018.05.008. eCollection 2018. PubMed PMID: 30182050; PubMed Central PMCID: PMC6121113. 9: Garcia-Carbonero N, Li W, Cabeza-Morales M, Martinez-Useros J, Garcia-Foncillas J. New Hope for Pancreatic Ductal Adenocarcinoma Treatment Targeting Endoplasmic Reticulum Stress Response: A Systematic Review. Int J Mol Sci. 2018 Aug 21;19(9). pii: E2468. doi: 10.3390/ijms19092468. Review. PubMed PMID: 30134550; PubMed Central PMCID: PMC6165247. 10: Bang BE, Malla N, Bhagwat SS, Aasmoe L, Winberg JO. A Sensitive Assay for Proteases in Bioaerosol Samples: Characterization and Quantification of Airborne Proteases in Salmon Industry Work Environments. Ann Work Expo Health. 2018 Oct 15;62(8):942-952. doi: 10.1093/annweh/wxy050. PubMed PMID: 29947734. 11: Ercan P, El SN. Bioaccessibility and inhibitory effects on digestive enzymes of carnosic acid in sage and rosemary. Int J Biol Macromol. 2018 Aug;115:933-939. doi: 10.1016/j.ijbiomac.2018.04.139. Epub 2018 Apr 28. PubMed PMID: 29709538. 12: Jiang HW, Czajkowsky DM, Wang T, Wang XD, Wang JB, Zhang HN, Liu CX, Wu FL, He X, Xu ZW, Chen H, Guo SJ, Li Y, Bi LJ, Deng JY, Xie J, Pei JF, Zhang XE, Tao SC. Identification of Serine 119 as an Effective Inhibitor Binding Site of M. tuberculosis Ubiquitin-like Protein Ligase PafA Using Purified Proteins and M. smegmatis. EBioMedicine. 2018 Apr;30:225-236. doi: 10.1016/j.ebiom.2018.03.025. Epub 2018 Mar 27. PubMed PMID: 29622495; PubMed Central PMCID: PMC5952411. 13: Limón D, Fábrega MJ, Calpena AC, Badia J, Baldomà L, Pérez-García L. Multifunctional Serine Protease Inhibitor-Coated Water-Soluble Gold Nanoparticles as a Novel Targeted Approach for the Treatment of Inflammatory Skin Diseases. Bioconjug Chem. 2018 Apr 18;29(4):1060-1072. doi: 10.1021/acs.bioconjchem.7b00717. Epub 2018 Feb 23. PubMed PMID: 29406699. 14: Van der Gucht W, Leemans A, De Schryver M, Heykers A, Caljon G, Maes L, Cos P, Delputte PL. Respiratory syncytial virus (RSV) entry is inhibited by serine protease inhibitor AEBSF when present during an early stage of infection. Virol J. 2017 Aug 17;14(1):157. doi: 10.1186/s12985-017-0824-3. PubMed PMID: 28818113; PubMed Central PMCID: PMC5561636. 15: Vieira SM, da Rocha SLG, Neves-Ferreira AGDC, Almeida RV, Perales J. Heterologous expression of the antimyotoxic protein DM64 in Pichia pastoris. PLoS Negl Trop Dis. 2017 Jul 31;11(7):e0005829. doi: 10.1371/journal.pntd.0005829. eCollection 2017 Jul. PubMed PMID: 28759578; PubMed Central PMCID: PMC5552330. 16: Chai HJ, Kiew LV, Chin Y, Norazit A, Mohd Noor S, Lo YL, Looi CY, Lau YS, Lim TM, Wong WF, Abdullah NA, Abdul Sattar MZ, Johns EJ, Chik Z, Chung LY. Renal targeting potential of a polymeric drug carrier, poly-l-glutamic acid, in normal and diabetic rats. Int J Nanomedicine. 2017 Jan 13;12:577-591. doi: 10.2147/IJN.S111284. eCollection 2017. PubMed PMID: 28144140; PubMed Central PMCID: PMC5245978. 17: Funato S, Yasuhara R, Yoshimura K, Miyamoto Y, Kaneko K, Suzawa T, Chikazu D, Mishima K, Baba K, Kamijo R. Extracellular matrix loss in chondrocytes after exposure to interleukin-1β in NADPH oxidase-dependent manner. Cell Tissue Res. 2017 Apr;368(1):135-144. doi: 10.1007/s00441-016-2551-2. Epub 2017 Jan 9. PubMed PMID: 28070636. 18: Harinath BC. Mycobacterial excretory secretory-31 protein with serine protease and lipase activities: An immunogen and drug target against tuberculosis infection. Int J Mycobacteriol. 2016 Dec;5 Suppl 1:S86-S87. doi: 10.1016/j.ijmyco.2016.09.065. Epub 2016 Nov 11. PubMed PMID: 28043634. 19: Akbar SM, Sharma HC. Alkaline serine proteases from Helicoverpa armigera: potential candidates for industrial applications. Arch Insect Biochem Physiol. 2017 Jan;94(1). doi: 10.1002/arch.21367. Epub 2016 Dec 26. PubMed PMID: 28019702. 20: Wang K, Yao Y, Zhu X, Zhang K, Zhou F, Zhu L. Amyloid β induces NLRP3 inflammasome activation in retinal pigment epithelial cells via NADPH oxidase- and mitochondria-dependent ROS production. J Biochem Mol Toxicol. 2017 Jun;31(6). doi: 10.1002/jbt.21887. Epub 2016 Dec 22. PubMed PMID: 28004443.