CAS No. : 192755-52-5

Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:M034379
Molecular Formula:C26H29N5O7
Molecular Weight:523.546
Target:IL-1beta converting enzyme inhibitor
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Appearance:Solid powder
Purity: > 98%
Cat No:M034379
Cas No:192755-52-5
IUPAC Name:(4S,7S)-N-[(2R,3S)-2-ethoxy-5-oxooxolan-3-yl]-7-(isoquinoline-1-carbonylamino)-6,10-dioxo-2,3,4,7,8,9-hexahydro-1H-pyridazino[1,2-a]diazepine-4-carboxamide
Pralnacasan is a caspase 1 (IL-1beta converting enzyme) inhibitor potentially for the treatment of osteoarthritis.

1: Bauer C, Loher F, Dauer M, Mayer C, Lehr HA, Schönharting M, Hallwachs R, Endres S, Eigler A. The ICE inhibitor pralnacasan prevents DSS-induced colitis in C57BL/6 mice and suppresses IP-10 mRNA but not TNF-alpha mRNA expression. Dig Dis Sci. 2007 Jul;52(7):1642-52. PubMed PMID: 17393315.
2: Loher F, Bauer C, Landauer N, Schmall K, Siegmund B, Lehr HA, Dauer M, Schoenharting M, Endres S, Eigler A. The interleukin-1 beta-converting enzyme inhibitor pralnacasan reduces dextran sulfate sodium-induced murine colitis and T helper 1 T-cell activation. J Pharmacol Exp Ther. 2004 Feb;308(2):583-90. PubMed PMID: 14610233.
3: Rudolphi K, Gerwin N, Verzijl N, van der Kraan P, van den Berg W. Pralnacasan, an inhibitor of interleukin-1beta converting enzyme, reduces joint damage in two murine models of osteoarthritis. Osteoarthritis Cartilage. 2003 Oct;11(10):738-46. PubMed PMID: 13129693.
4: Siegmund B, Zeitz M. Pralnacasan (vertex pharmaceuticals). IDrugs. 2003 Feb;6(2):154-8. Review. PubMed PMID: 12789619.
5: Handy EL, Totaro KA, Lin CP, Sello JK. Efficient and regiospecific syntheses of peptides with piperazic and dehydropiperazic acids via a multicomponent reaction. Org Lett. 2014 Jul 3;16(13):3488-91. doi: 10.1021/ol501425b. PubMed PMID: 24937740.
6: Ravizza T, Lucas SM, Balosso S, Bernardino L, Ku G, Noé F, Malva J, Randle JC, Allan S, Vezzani A. Inactivation of caspase-1 in rodent brain: a novel anticonvulsive strategy. Epilepsia. 2006 Jul;47(7):1160-8. PubMed PMID: 16886979.
7: Riad A, Walther T, Yang J, Altmann C, Escher F, Westermann D, Spillmann F, Schultheiss HP, Tschöpe C. The cardiovascular influence of interleukin-1 beta on the expression of bradykinin B1 and B2 receptors. Int Immunopharmacol. 2008 Feb;8(2):222-30. doi: 10.1016/j.intimp.2007.07.027. PubMed PMID: 18182231.
8: Cornelis S, Kersse K, Festjens N, Lamkanfi M, Vandenabeele P. Inflammatory caspases: targets for novel therapies. Curr Pharm Des. 2007;13(4):367-85. Review. PubMed PMID: 17311555.
9: Timmermans K, van der Wal SE, Vaneker M, van der Laak JA, Netea MG, Pickkers P, Scheffer GJ, Joosten LA, Kox M. IL-1β processing in mechanical ventilation-induced inflammation is dependent on neutrophil factors rather than caspase-1. Intensive Care Med Exp. 2013 Dec;1(1):27. doi: 10.1186/2197-425X-1-8. PubMed PMID: 26266796; PubMed Central PMCID: PMC4797957.
10: Qian L, Zhang CJ, Wu J, Yao SQ. Fused Bicyclic Caspase-1 Inhibitors Assembled by Copper-Free Strain-Promoted Alkyne-Azide Cycloaddition (SPAAC). Chemistry. 2017 Jan 5;23(2):360-369. doi: 10.1002/chem.201603150. PubMed PMID: 27882694.
11: Bauer C, Duewell P, Mayer C, Lehr HA, Fitzgerald KA, Dauer M, Tschopp J, Endres S, Latz E, Schnurr M. Colitis induced in mice with dextran sulfate sodium (DSS) is mediated by the NLRP3 inflammasome. Gut. 2010 Sep;59(9):1192-9. doi: 10.1136/gut.2009.197822. PubMed PMID: 20442201.
12: Gotham S. Digestive Disease Week 2004. Bowel inflammation. IDrugs. 2004 Jun;7(6):516-9. PubMed PMID: 15197649.
13: Ross J, Brough D, Gibson RM, Loddick SA, Rothwell NJ. A selective, non-peptide caspase-1 inhibitor, VRT-018858, markedly reduces brain damage induced by transient ischemia in the rat. Neuropharmacology. 2007 Oct;53(5):638-42. PubMed PMID: 17845807.
14: Hauff K, Zamzow C, Law WJ, De Melo J, Kennedy K, Los M. Peptide-based approaches to treat asthma, arthritis, other autoimmune diseases and pathologies of the central nervous system. Arch Immunol Ther Exp (Warsz). 2005 Jul-Aug;53(4):308-20. Review. PubMed PMID: 16088315.
15: Linton SD. Caspase inhibitors: a pharmaceutical industry perspective. Curr Top Med Chem. 2005;5(16):1697-717. Review. PubMed PMID: 16375749.
16: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2003 Jan-Feb;25(1):53-76. PubMed PMID: 12690708.
17: Siegmund B. Interleukin-1beta converting enzyme (caspase-1) in intestinal inflammation. Biochem Pharmacol. 2002 Jul 1;64(1):1-8. Review. PubMed PMID: 12106600.
18: Leung-Toung R, Li W, Tam TF, Karimian K. Thiol-dependent enzymes and their inhibitors: a review. Curr Med Chem. 2002 May;9(9):979-1002. Review. PubMed PMID: 11966457.
19: Randle JC, Harding MW, Ku G, Schönharting M, Kurrle R. ICE/Caspase-1 inhibitors as novel anti-inflammatory drugs. Expert Opin Investig Drugs. 2001 Jul;10(7):1207-9. Review. PubMed PMID: 11772244.

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