Cipargamin (NITD609)

An antimalarial agent

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库存: 现货

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2mg

￥1087.00

870.00

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5mg

￥1937.00

1550.00

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10mg

￥3225.00

2580.00

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50mg

￥9625.00

7700.00

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100mg

￥15887.00

12710.00

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货号: ajce52080
CAS: 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
分子式: C19H14Cl2FN3O
分子量: 390.24
纯度: >98%
溶解度: DMSO : 50 mg/mL (128.13 mM);Water : < 0.1 mg/mL (insoluble)
储存: Store at -20°C
库存: 现货

Background

Cipargamin is an antimalarial agent.^1,2,3 It inhibits the Na⁺-ATPase activity of wild-type or mutant P. falciparum P-type ATPase (PfATP4; IC₅₀s = 12.3-13.9 and 21.1-32.5 nM, respectively, in P. falciparum membranes).¹ Cipargamin is active against the P. falciparum chloroquine-sensitive strain NF54 and chloroquine-resistant strain K1 (IC₅₀s = 0.5 and 0.6 nM, respectively).² It reduces parasitemia and increases survival in a mouse model of P. berghei infection when administered at doses of 10, 30, and 100 mg/kg.³

1.Rosling, J.E.O., Ridgway, M.C., Summers, R.L., et al.Biochemical characterization and chemical inhibition of PfATP4-associated Na+-ATPase activity in Plasmodium falciparum membranesJ. Biol. Chem.293(34)13327-13337(2018) 2.van Pelt-Koops, J.C., Pett, H.E., Graumans, W., et al.The spiroindolone drug candidate NITD609 potently inhibits gametocytogenesis and blocks Plasmodium falciparum transmission to Anopheles mosquito vectorAntimicrob. Agents Chemother.56(7)3544-3548(2012) 3.Rottmann, M., McNamara, C., Yeung, B.K.S., et al.Spiroindolones, a potent compound class for the treatment of malariaScience329(5996)1175-1180(2010)