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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
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Cipargamin (NITD609) (NITD609) 是一种有效的抗疟化合物，对疟原虫的 IC50 约为 1 nM。
Cas No.1193314-23-6
别名(1'R,3'S)-5,7'-二氯-6'-氟-2',3',4',9'-四氢-3'-甲基螺[3H-吲哚-3,1'-[1H]吡啶并[3,4-B]吲哚]-2(1H)-酮,NITD609; KAE609
Canonical SMILESFC1=C(Cl)C=C(NC2=C3C[C@H](C)N[C@@]2(C4=C(C=CC(Cl)=C4)N5)C5=O)C3=C1
分子式C19H14Cl2FN3O
分子量390.24
溶解度DMSO : 50 mg/mL (128.13 mM);Water :< 0.1 mg/mL (insoluble)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.