Cipargamin是一种有效的抗疟药物,对恶性疟原虫的IC50值约为 1 nM。
产品描述
Cipargamin is an effective antimalarial compound. It has an IC50 of appr 1 nM against P. falciparum.
体外活性
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].
体内活性
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].
Cas No.
1193314-23-6
分子式
C19H14Cl2FN3O
分子量
390.24
别名
NITD609;KAE609;Cipargamin
储存和溶解度
H2O:< 0.1 mg/mL (insoluble)
DMSO:50 mg/mL (128.13 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years