Name | (3R,3'S)-5,7'-dichloro-6'-fluoro-3'-methylspiro[1H-indole-3,1'-2,3,4,9-tetrahydropyrido[3,4-b]indole]-2-one |
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Synonyms |
(1R,3S)-5',7-Dichloro-6-fluoro-3-methyl-2,3,4,9-tetrahydrospiro[β-carboline-1,3'-indol]-2'(1'H)-one
NITD609 cipargamin nitd 609 Spiro[3H-indole-3,1'-[1H]pyrido[3,4-b]indol]-2(1H)-one, 5,7'-dichloro-6'-fluoro-2',3',4',9'-tetrahydro-3'-methyl-, (3R,3'S)- KAE609 |
Description | Cipargamin (NITD609) is an potent antimalarial compound, with IC50 of appr 1 nM against P. falciparum. |
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Related Catalog | |
Target |
IC50: 1 nM (P. falciparum)[3] |
In Vitro | Cipargamin (NITD609) inhibits T. gondii with a MIC90 for tachyzoites of 5 μM and a MIC50 of 1 μM, without toxicity to human foreskin fibroblasts (HFFs) at the highest concentration tested (10 μM)[1]. Cipargamin (NITD609) is the most effective inhibitor of early gametocyte development at 50 and 500 nM. Cipargamin shows a dose-dependent inhibiting effect on late gametocyte development[2]. Cipargamin (NITD609) shows potent activities against a panel of culture-adapted P. falciparum strains, with ICIC50 values of 0.5-1.4 nM. Cipargamin is effective as artesunate with potency in the low nanomolar range (ICIC50 values consistently <10 nM) against all P. falciparum and P. vivax isolates[3]. |
In Vivo | Cipargamin (NITD609) shows favorable pharmacokinetic properties and displays single dose cure efficacy in a malaria mouse model. Cipargamin (100 mg/kg) completely clears P. berghei infection in all treated mice, and partial cure (50%) is achieved with a single oral dose at 30 mg/kg[3]. |
References |
Density | 1.6±0.1 g/cm3 |
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Boiling Point | 621.3±55.0 °C at 760 mmHg |
Molecular Formula | C19H14Cl2FN3O |
Molecular Weight | 390.238 |
Flash Point | 329.6±31.5 °C |
Exact Mass | 389.049805 |
PSA | 60.41000 |
LogP | 4.61 |
Vapour Pressure | 0.0±1.8 mmHg at 25°C |
Index of Refraction | 1.738 |