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ACT-451840 is capable of eliminating both sensitive and resistant strains of Plasmodium falciparum and has the advantages of oral activity, potency, low toxicity, rapid onset of action in all asexual blood stages of Plasmodium, and a mechanism of action similar to that of artemisinin derivatives. In in vivo experiments, ACT-451840 showed excellent antimalarial effects at a dose of 30 mg/kg, with a parasite reduction rate of 99.80%.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $107 | In Stock | |
5 mg | $235 | In Stock | |
10 mg | $375 | In Stock | |
25 mg | $730 | In Stock | |
50 mg | $1,170 | In Stock | |
100 mg | $1,830 | In Stock | |
1 mL x 10 mM (in DMSO) | $245 | In Stock |
Description | ACT-451840 is capable of eliminating both sensitive and resistant strains of Plasmodium falciparum and has the advantages of oral activity, potency, low toxicity, rapid onset of action in all asexual blood stages of Plasmodium, and a mechanism of action similar to that of artemisinin derivatives. In in vivo experiments, ACT-451840 showed excellent antimalarial effects at a dose of 30 mg/kg, with a parasite reduction rate of 99.80%. |
In vitro | ACT-451840 has a 50% inhibitory concentration of 0.4 nM against the drug-susceptible P. falciparum NF54 strain; ACT-451840 effectively blocks male gamete formation from the gametocyte stage at a 50% inhibitory concentration of 5.89 nM, and blocks mosquito oocyst development in a dose-dependent manner at a 50% inhibitory concentration of 30 nM. [2] |
In vivo | In the in vivo efficacy model, the 90% effective dose against P. falciparum of ACT-451840 was 3.7 mg/kg and the 90% effective dose against P. berghei was 13 mg/kg. |
Alias | ACT451840 |
Molecular Weight | 750.97 |
Formula | C47H54N6O3 |
Cas No. | 1984890-99-4 |
Smiles | CC(=O)N1CCN(CC1)c1ccc(CN([C@@H](Cc2ccccc2)C(=O)N2CCN(Cc3ccc(cc3)C#N)CC2)C(=O)\C=C\c2ccc(cc2)C(C)(C)C)cc1 |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
Solubility Information | DMSO: 30.00 mg/mL (39.95 mM), Sonication is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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