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Cipargamin

Catalog No. T16326   CAS 1193314-23-6
Synonyms: KAE609, NITD609

Cipargamin (NITD609) is an effective antimalarial compound. It has an IC50 of appr 1 nM against P. falciparum.

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Cipargamin Chemical Structure
Cipargamin, CAS 1193314-23-6
Pack Size Availability Price/USD Quantity
1 mg In stock $ 53.00
2 mg In stock $ 76.00
5 mg In stock $ 142.00
10 mg In stock $ 228.00
25 mg In stock $ 438.00
50 mg In stock $ 743.00
100 mg In stock $ 1,190.00
200 mg In stock $ 1,580.00
500 mg In stock $ 2,380.00
1 mL * 10 mM (in DMSO) In stock $ 157.00
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Purity: 98.58%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Cipargamin (NITD609) is an effective antimalarial compound. It has an IC50 of appr 1 nM against P. falciparum.
Targets&IC50 P. falciparum:1 nM
In vitro Cipargamin is the most effective inhibitor of early gametocyte development at 50 and 500 nM. Cipargamin displays a dose-dependent inhibiting effect on late gametocyte development. Cipargamin inhibits T. gondii with an MIC90 for tachyzoites of 5 μM and an MIC50 of 1 μM. At the highest concentration tested (10 μM), It has no toxicity to human foreskin fibroblasts (HFFs). Cipargamin shows effective activities against a panel of culture-adapted P. falciparum strains (IC50: 0.5-1.4 nM). Cipargamin is effective as an artesunate with potency in the low nanomolar range (ICIC50 values consistently <10 nM) against all P. falciparum and P. vivax isolates [1][2][3].
In vivo Cipargamin (100 mg/kg) fully clears P. berghei infection in all treated mice, and partial cure (50%) is achieved with a single oral dose at 30 mg/kg. Cipargamin displays favorable pharmacokinetic properties and shows single-dose cure efficacy in a malaria mouse model [3].
Synonyms KAE609, NITD609
Molecular Weight 390.24
Formula C19H14Cl2FN3O
CAS No. 1193314-23-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 0.1 mg/mL (insoluble)

DMSO: 55 mg/mL (140.94 mM), Sonication is recommended.

TargetMolReferences and Literature

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.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Parasitic Compound Library Drug Repurposing Compound Library Pediatric Drug Library NO PAINS Compound Library Bioactive Compounds Library Max Bioactive Compound Library Clinical Compound Library Anti-Infection Compound Library

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Keywords

Cipargamin 1193314-23-6 Microbiology/Virology Parasite inhibit KAE609 KAE-609 NITD-609 NITD 609 Inhibitor NITD609 KAE 609 inhibitor

 

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