Name | ACT-451840 |
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Synonyms |
(2E)-N-[4-(4-Acetyl-1-piperazinyl)benzyl]-N-{(2S)-1-[4-(4-cyanobenzyl)-1-piperazinyl]-1-oxo-3-phenyl-2-propanyl}-3-[4-(2-methyl-2-propanyl)phenyl]acrylamide
2-Propenamide, N-[[4-(4-acetyl-1-piperazinyl)phenyl]methyl]-N-[(1S)-2-[4-[(4-cyanophenyl)methyl]-1-piperazinyl]-2-oxo-1-(phenylmethyl)ethyl]-3-[4-(1,1-dimethylethyl)phenyl]-, (2E)- ACT-451840 MFCD31700747 |
Description | ACT-451840 is an orally active, potent and low-toxicity compound, showing activity against sensitive and resistant plasmodium falciparum strains. ACT-451840 targets all asexual blood stages of the parasite, has a rapid onset of action. ACT-451840 behaves in a way similar to artemisinin derivatives, with very rapid onset of action and elimination of parasite. ACT-451840 can be used for the research of malarial[1][2][3]. |
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Related Catalog | |
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. |
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]. |
References |
Density | 1.2±0.1 g/cm3 |
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Boiling Point | 953.8±65.0 °C at 760 mmHg |
Molecular Formula | C47H54N6O3 |
Molecular Weight | 750.97 |
Flash Point | 530.6±34.3 °C |
Exact Mass | 750.425720 |
LogP | 6.74 |
Vapour Pressure | 0.0±0.3 mmHg at 25°C |
Index of Refraction | 1.652 |