2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Biological activity
Description
CAS NO.：1984890-99-4 Product Name：ACT-451840 Synonyms：SB18671;N-[[4-(4-acetylpiperazin-1-yl)phenyl]methyl]-3-(4-tert-butylphenyl)-N-[1-[4-[(4-cyanophenyl)methyl]p;ACT-451840 EINEC: Molecular Formula：C47H54N6O3 Molecular Weight：750.970071315765
Target:
In Vivo
ACT-451840 (10 and 60 mg kg) starts to show significant antimalarial effects (parasite reduction) in vivo at 20 mg/kg. ACT-451840 exhibits curative activity at 300 mg/kg and significant antimalarial effects already at 100 mg/kg. ACT-451840 shows excellent reduction at 30 mg/kg, resulting in 99.80 % activity[2]. ACT-451840 shows efficacy in the Plasmodium berghei mouse model[2].
In Vitro
ACT-451840 shows a 50 % inhibition concentration of 0.4 nM against the drug-sensitive P. falciparum NF54 strain. The IC50 value of ACT-451840 against the murine malaria parasite P. berghei is 13.5 nM in in vitro ex vivo assays.
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Bruderer S, et al. First-in-humans study of the safety, tolerability, and pharmacokinetics of ACT-451840, a new chemical entity with antimalarial activity. Antimicrob Agents Chemother. 2015;59(2):935-942.
[2]. Boss C, et al. Discovery and Characterization of ACT-451840: an Antimalarial Drug with a Novel Mechanism of Action. ChemMedChem. 2016;11(18):1995-2014.
[3]. Le Bihan A, et al. Characterization of Novel Antimalarial Compound ACT-451840: Preclinical Assessment of Activity and Dose-Efficacy Modeling. PLoS Med. 2016;13(10):e1002138. Published 2016 Oct 4.
Return Policy
If you are in any way unsatisfied with your purchase, you may return any item(s) within 365 days of its original purchase date.
Please provide your Order Number in the email. We strive to reply to all email inquiries within one business day.
