DC Chemicals Limited
China
Product Name: NITD 609
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Purity: 98.0%
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1193314-23-6

1193314-23-6 structure

1193314-23-6 structure

Name: NITD-609
Chemical Name: (3R,3'S)-5,7'-dichloro-6'-fluoro-3'-methylspiro[1H-indole-3,1'-2,3,4,9-tetrahydropyrido[3,4-b]indole]-2-one
CAS Number: 1193314-23-6
Molecular Formula: C₁₉H₁₄Cl₂FN₃O
Molecular Weight: 390.238
Catalog: Signaling Pathways Anti-infection Parasite
Create Date: 2017-08-05 07:46:12
Modify Date: 2024-01-02 10:13:00
Cipargamin (NITD609) is an potent antimalarial compound, with IC50 of appr 1 nM against P. falciparum.

Name	(3R,3'S)-5,7'-dichloro-6'-fluoro-3'-methylspiro[1H-indole-3,1'-2,3,4,9-tetrahydropyrido[3,4-b]indole]-2-one
Synonyms	(1R,3S)-5',7-Dichloro-6-fluoro-3-methyl-2,3,4,9-tetrahydrospiro[β-carboline-1,3'-indol]-2'(1'H)-one NITD609 cipargamin nitd 609 Spiro[3H-indole-3,1'-[1H]pyrido[3,4-b]indol]-2(1H)-one, 5,7'-dichloro-6'-fluoro-2',3',4',9'-tetrahydro-3'-methyl-, (3R,3'S)- KAE609

Description	Cipargamin (NITD609) is an potent antimalarial compound, with IC50 of appr 1 nM against P. falciparum.
Related Catalog	Signaling Pathways >> Anti-infection >> Parasite Research Areas >> Infection
Target	IC50: 1 nM (P. falciparum)[3]
In Vitro	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 <10 nM) against all P. falciparum and P. vivax isolates[3].
In Vivo	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].
References	[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.

Density	1.6±0.1 g/cm3
Boiling Point	621.3±55.0 °C at 760 mmHg
Molecular Formula	C₁₉H₁₄Cl₂FN₃O
Molecular Weight	390.238
Flash Point	329.6±31.5 °C
Exact Mass	389.049805
PSA	60.41000
LogP	4.61
Vapour Pressure	0.0±1.8 mmHg at 25°C
Index of Refraction	1.738