ACT-451840

TargetMol
Product Code: TAR-T23625
Supplier: TargetMol
CodeSizePrice
TAR-T23625-5mg5mg£250.00
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Quantity:
TAR-T23625-50mg50mg£962.00
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Quantity:
TAR-T23625-100mg100mg£1,468.00
Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here.
Quantity:
Prices exclude any Taxes / VAT

Overview

Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20℃

Images

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Further Information

Bioactivity:
ACT-451840 is a drug of antimalarial activity. It has effective activity against sensitive and resistant Plasmodium falciparum strains.
CAS:
1839508-99-4
Formula:
C47H54N6O3
Molecular Weight:
750.988
Purity:
0.98
SMILES:
CC(=O)N1CCN(CC1)c1ccc(CN([C@@H](Cc2ccccc2)C(=O)N2CCN(Cc3ccc(cc3)C#N)CC2)C(=O)C=Cc2ccc(cc2)C(C)(C)C)cc1

References

1. Bruderer S, Hurst N, de Kanter R, Miraval T, Pfeifer T, Donazzolo Y, Dingemanse J. First-in-humans study of the safety, tolerability, and pharmacokinetics of ACT-451840, a new chemical entity with antimalarial activity. Antimicrob Agents Chemother. 2015 Feb;59(2):935-42. doi: 10.1128/AAC.04125-14. Epub 2014 Nov 24. PubMed PMID: 25421475; PubMed Central PMCID: PMC4335896. 2. Le Bihan A, de Kanter R, Angulo-Barturen I, et al. Characterization of Novel Antimalarial Compound ACT-451840: Preclinical Assessment of Activity and Dose-Efficacy Modeling. PLoS Med. 2016 Oct 4;13(10):e1002138. doi: 10.1371/journal.pmed.1002138. eCollection 2016 Oct. PubMed PMID: 27701420; PubMed Central PMCID: PMC5049785. 3. Ng CL, Siciliano G, Lee MC, de Almeida MJ, Corey VC, Bopp SE, Bertuccini L, Wittlin S, Kasdin RG, Le Bihan A, Clozel M, Winzeler EA, Alano P, Fidock DA. CRISPR-Cas9-modified pfmdr1 protects Plasmodium falciparum asexual blood stages and gametocytes against a class of piperazine-containing compounds but potentiates artemisinin-based combination therapy partner drugs. Mol Microbiol. 2016 Aug;101(3):381-93. doi: 10.1111/mmi.13397. Epub 2016 May 7. PubMed PMID: 27073104; PubMed Central PMCID: PMC4958522. 4. Boss C, Aissaoui H, Amaral N, Bauer A, Bazire S, Binkert C, Brun R, B?rki 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. Discovery and Characterization of ACT-451840: an Antimalarial Drug with a Novel Mechanism of Action. ChemMedChem. 2016 Sep 20;11(18):1995-2014. doi: 10.1002/cmdc.201600298. Epub 2016 Jul 29. PubMed PMID: 27471138.