For research use only. Not for therapeutic Use.
Cipargamin (KAE609)（Cat No.:I006138）is a novel antimalarial agent with potent activity against Plasmodium species, including multidrug-resistant strains. It targets the Plasmodium P-type ATPase 4 (PfATP4), a crucial ion pump involved in sodium homeostasis, leading to disrupted parasite metabolism and death. Cipargamin is effective against blood-stage parasites and demonstrates rapid parasite clearance. Its favorable pharmacokinetics and oral bioavailability make it a promising candidate for malaria treatment. Currently in clinical trials, Cipargamin represents a significant advancement in combating malaria, addressing the global challenge of drug-resistant infections.
| Catalog Number | I006138 |
| CAS Number | 1193314-23-6 |
| Synonyms | NITD609, NITD 609, NITD-609, KAE609, KAE 609, KAE-609, GNF-609; GNF 609; GNF609; Cipargamin.;(1R,3S)-5’,7-Dichloro-6-fluoro-3-methyl-spiro[2,3,4,9-tetrahydropyrido[3,4-b]indole-1,3’-indoline]-2’-one |
| Molecular Formula | C19H14Cl2FN3O |
| Purity | ≥95% |
| Target | Parasite |
| Solubility | Soluble in DMSO, not in water |
| Storage | Store at -20°C |
| IUPAC 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 |
| InChI | InChI=1S/C19H14Cl2FN3O/c1-8-4-11-10-6-14(22)13(21)7-16(10)23-17(11)19(25-8)12-5-9(20)2-3-15(12)24-18(19)26/h2-3,5-8,23,25H,4H2,1H3,(H,24,26)/t8-,19+/m0/s1 |
| InChIKey | CKLPLPZSUQEDRT-WPCRTTGESA-N |
| SMILES | C[C@H]1CC2=C([C@]3(N1)C4=C(C=CC(=C4)Cl)NC3=O)NC5=CC(=C(C=C25)F)Cl |
| Reference | </br>1:Estimation of the In Vivo MIC of Cipargamin in Uncomplicated Plasmodium falciparum Malaria. Hien TT, White NJ, Thuy-Nhien NT, Hoa NT, Thuan PD, Tarning J, Nosten F, Magnusson B, Jain JP, Hamed K.Antimicrob Agents Chemother. 2017 Jan 24;61(2). pii: e01940-16. doi: 10.1128/AAC.01940-16. Print 2017 Feb. PMID: 27872070 Free PMC Article</br>2:Comparative chemical genomics reveal that the spiroindolone antimalarial KAE609 (Cipargamin) is a P-type ATPase inhibitor. Goldgof GM, Durrant JD, Ottilie S, Vigil E, Allen KE, Gunawan F, Kostylev M, Henderson KA, Yang J, Schenken J, LaMonte GM, Manary MJ, Murao A, Nachon M, Stanhope R, Prescott M, McNamara CW, Slayman CW, Amaro RE, Suzuki Y, Winzeler EA.Sci Rep. 2016 Jun 13;6:27806. doi: 10.1038/srep27806. PMID: 27291296 Free PMC Article</br>3:KAE609 (Cipargamin), a New Spiroindolone Agent for the Treatment of Malaria: Evaluation of the Absorption, Distribution, Metabolism, and Excretion of a Single Oral 300-mg Dose of [14C]KAE609 in Healthy Male Subjects. Huskey SE, Zhu CQ, Fredenhagen A, Kühnöl J, Luneau A, Jian Z, Yang Z, Miao Z, Yang F, Jain JP, Sunkara G, Mangold JB, Stein DS.Drug Metab Dispos. 2016 May;44(5):672-82. doi: 10.1124/dmd.115.069187. Epub 2016 Feb 26. PMID: 26921387 Free Article</br>4:Open-label, single-dose, parallel-group study in healthy volunteers to determine the drug-drug interaction potential between KAE609 (cipargamin) and piperaquine. Stein DS, Jain JP, Kangas M, Lefèvre G, Machineni S, Griffin P, Lickliter J.Antimicrob Agents Chemother. 2015;59(6):3493-500. doi: 10.1128/AAC.00340-15. Epub 2015 Apr 6. PMID: 25845867 Free PMC Article</br>5:A first-in-human randomized, double-blind, placebo-controlled, single- and multiple-ascending oral dose study of novel antimalarial Spiroindolone KAE609 (Cipargamin) to assess its safety, tolerability, and pharmacokinetics in healthy adult volunteers. Leong FJ, Li R, Jain JP, Lefèvre G, Magnusson B, Diagana TT, Pertel P.Antimicrob Agents Chemother. 2014 Oct;58(10):6209-14. doi: 10.1128/AAC.03393-14. Epub 2014 Aug 11. PMID: 25114127 Free PMC Article |
