Cipargamin

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Cipargamin (KAE609、NITD609) 是一种速效、强效抗疟药，可在体外抑制一组培养适应的恶性疟原虫菌株的血液阶段活性，IC50 为 0.5-1.4 nM。

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; 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; 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.Parasite Infection Phase 2 Clinical.

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). 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. 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.

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.

KAE609 | NITD609

Microbiology/Virology

Parasite

Parasite

Infection

Parasite Infection

1193314-23-6

390.239

C19H14Cl2FN3O

>98% (HPLC)

DMSO : 50 mg/mL 128.13 mM;H2O : < 0.1 mg/mL

O=C([C@]12N[C@@H](C)CC3=C1NC4=C3C=C(F)C(Cl)=C4)NC5=C2C=C(Cl)C=C5

(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

(-20℃)

With Ice Pack

≥ 2 years