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Cipargamin

Chemical Structure : Cipargamin

CAS No.: 1193314-23-6

Cipargamin (KAE609, NITD609)

Catalog No.: PC-63378Not For Human Use, Lab Use Only.

Cipargamin (KAE609, NITD609) is a fast-acting, potent antimalarial agent that inhibits blood-stage activity in vitro against a panel of culture-adapted P. falciparum strains with IC50 of 0.5-1.4 nM.

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Biological Activity

Cipargamin (KAE609, NITD609) is a fast-acting, potent antimalarial agent that inhibits blood-stage activity in vitro against a panel of culture-adapted P. falciparum strains with IC50 of 0.5-1.4 nM.
NITD609 inhibits the early and late development of Plasmodium falciparum gametocytes in vitro in a dose-dependent fashion over a range of 5 to 500 nM.
NITD609 also is a very effective drug in reducing transmission to the Anopheles stephensi mosquito vector; shows pharmacokinetic properties compatible with once-daily oral dosing and has single-dose efficacy in rodent malaria model.

Physicochemical Properties

M.Wt 390.239
Formula C19H14Cl2FN3O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(1'R,3'S)-5,7'-Dichloro-6'-fluoro-2',3',4',9'-tetrahydro-3'-methylspiro[3H-indole-3,1'-[1H]pyrido[3,4-b]indol]-2(1H)-one

References

1. Rottmann M, et al. Science. 2010 Sep 3;329(5996):1175-80.

2. van Pelt-Koops JC, et al. Antimicrob Agents Chemother. 2012 Jul;56(7):3544-8.

3. Spillman NJ, et al. Cell Host Microbe. 2013 Feb 13;13(2):227-37.

4. Zhou Y, et al. Antimicrob Agents Chemother. 2014;58(3):1789-92.

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