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Cipargamin(NITD609)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Cipargamin(NITD609)图片
CAS NO:1193314-23-6
规格:98%
分子量:390.24
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Cipargamin(NITD609)是一种有效的抗疟疾药,对恶性疟原虫的IC50值约为1nM。
CAS:1193314-23-6
分子式:C19H14Cl2FN3O
分子量:390.24
纯度:98%
存储:Store at -20°C

Background:

Cipargamin (NITD609) is an potent antimalarial compound, with IC50 of appr 1 nM against P. falciparum.


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 P. falciparum and P. vivax isolates[3].


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].


[1]. Zhou Y, et al. Spiroindolone that inhibits PfATPase4 is a potent, cidal inhibitor of Toxoplasma gondii tachyzoites in vitro and in vivo. Antimicrob Agents Chemother. 2014;58(3):1789-92. [2]. van Pelt-Koops JC, et al. The spiroindolone drug candidate NITD609 potently inhibits gametocytogenesis and blocks Plasmodium falciparum transmission to anopheles mosquito vector. Antimicrob Agents Chemother. 2012 Jul;56(7):3544-8. [3]. Rottmann M, et al. Spiroindolones, a potent compound class for the treatment of malaria. Science. 2010 Sep 3;329(5996):1175-80.