ACT-451840


CAS No. : 1314143-88-8

ACT-451840,1314143-88-8
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000353
Synonyms:ACT-451840; ACT 451840; ACT451840;(S,E)-N-(4-(4-acetylpiperazin-1-yl)benzyl)-3-(4-(tert-butyl)phenyl)-N-(1-(4-(4-cyanobenzyl)piperazin-1-yl)-1-oxo-3-phenylpropan-2-yl)acrylamide
Molecular Formula:C47H54N6O3
Molecular Weight:750.988
Target:Aspartic Endopeptidase Inhibitor
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Appearance:Solid powder
Purity: > 98%
Cat No:I000353
Cas No:1314143-88-8
Product-Name:ACT-451840
InChI:InChI=1S/C47H54N6O3/c1-36(54)50-28-30-51(31-29-50)43-21-16-41(17-22-43)35-53(45(55)23-18-37-14-19-42(20-15-37)47(2,3)4)44(32-38-8-6-5-7-9-38)46(56)52-26-24-49(25-27-52)34-40-12-10-39(33-48)11-13-40/h5-23,44H,24-32,34-35H2,1-4H3/b23-18+/t44-/m0/s1
InChIKey:BQZUYCCCNXOADJ-TVNMEPFQSA-N
SMILES:O=C(N(CC1=CC=C(N2CCN(C(C)=O)CC2)C=C1)[C@@H](CC3=CC=CC=C3)C(N4CCN(CC5=CC=C(C#N)C=C5)CC4)=O)/C=C/C6=CC=C(C(C)(C)C)C=C6
ACT-451840 is an aspartic endopeptidase inhibitor with potent activity against sensitive and resistant Plasmodium falciparum strains. The dual activity of ACT-451840 against asexual and sexual stages of P. falciparum and the activity on P. vivax have the potential to meet the specific profile of a target compound that could replace the fast-acting artemisinin component and harbor additional gametocytocidal activity and, thereby, transmission-blocking properties. The fast parasite reduction ratio (PRR) and gametocytocidal effect of ACT-451840 were recently also confirmed in a clinical proof-of-concept (POC) study. ACT-451840 is a potential treatment for malaria.

1:Characterization of Novel Antimalarial Compound ACT-451840: Preclinical Assessment of Activity and Dose-Efficacy Modeling. Le Bihan A, de Kanter R, Angulo-Barturen I, Binkert C, Boss C, Brun R, Brunner R, Buchmann S, Burrows J, Dechering KJ, Delves M, Ewerling S, Ferrer S, Fischli C, Gamo-Benito FJ, Gnädig NF, Heidmann B, Jiménez-Díaz MB, Leroy D, Martínez MS, Meyer S, Moehrle JJ, Ng CL, Noviyanti R, Ruecker A, Sanz LM, Sauerwein RW, Scheurer C, Schleiferboeck S, Sinden R, Snyder C, Straimer J, Wirjanata G, Marfurt J, Price RN, Weller T, Fischli W, Fidock DA, Clozel M, Wittlin S.PLoS Med. 2016 Oct 4;13(10):e1002138. doi: 10.1371/journal.pmed.1002138. eCollection 2016 Oct. PMID: 27701420 Free PMC Article
2:Discovery and Characterization of ACT-451840: an Antimalarial Drug with a Novel Mechanism of Action. Boss C, Aissaoui H, Amaral N, Bauer A, Bazire S, Binkert C, Brun R, Bürki C, Ciana CL, Corminboeuf O, Delahaye S, Dollinger C, Fischli C, Fischli W, Flock A, Frantz MC, Girault M, Grisostomi C, Friedli A, Heidmann B, Hinder C, Jacob G, Le Bihan A, Malrieu S, Mamzed S, Merot A, Meyer S, Peixoto S, Petit N, Siegrist R, Trollux J, Weller T, Wittlin S.ChemMedChem. 2016 Sep 20;11(18):1995-2014. doi: 10.1002/cmdc.201600298. Epub 2016 Jul 29. PMID: 27471138
3:First-in-humans study of the safety, tolerability, and pharmacokinetics of ACT-451840, a new chemical entity with antimalarial activity. Bruderer S, Hurst N, de Kanter R, Miraval T, Pfeifer T, Donazzolo Y, Dingemanse J.Antimicrob Agents Chemother. 2015 Feb;59(2):935-42. doi: 10.1128/AAC.04125-14. Epub 2014 Nov 24. PMID: 25421475 Free PMC Article
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