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Cipargamin
CAS No. 1193314-23-6
Cipargamin( KAE609 | NITD609 )
Catalog No. M10671 CAS No. 1193314-23-6
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.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 89 | In Stock |
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| 5MG | 81 | In Stock |
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| 10MG | 130 | In Stock |
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| 25MG | 250 | In Stock |
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| 50MG | 415 | In Stock |
|
| 100MG | 663 | In Stock |
|
| 200MG | 882 | In Stock |
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| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
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Biological Information
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Product NameCipargamin
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NoteResearch use only, not for human use.
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Brief DescriptionCipargamin (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.
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DescriptionCipargamin (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.
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In VitroCipargamin (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.
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In VivoCipargamin (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.
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SynonymsKAE609 | NITD609
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PathwayMicrobiology/Virology
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TargetParasite
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RecptorParasite
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Research AreaInfection
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IndicationParasite Infection
Chemical Information
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CAS Number1193314-23-6
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Formula Weight390.239
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Molecular FormulaC19H14Cl2FN3O
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Purity>98% (HPLC)
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SolubilityDMSO : 50 mg/mL 128.13 mM;H2O : < 0.1 mg/mL
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SMILESO=C([C@]12N[C@@H](C)CC3=C1NC4=C3C=C(F)C(Cl)=C4)NC5=C2C=C(Cl)C=C5
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Chemical Name(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
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Rottmann M, et al. Science. 2010 Sep 3;329(5996):1175-80.
2. van Pelt-Koops JC, et al. Antimicrob Agents Chemother. 2012 Jul;56(7):3544-8.
3. Spillman NJ, et al. Cell Host Microbe. 2013 Feb 13;13(2):227-37.
4. Zhou Y, et al. Antimicrob Agents Chemother. 2014;58(3):1789-92.
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