产品
编 号:F555297
分子式:C10H11BO4
分子量:206
产品类型
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CAS No: 1268335-33-6
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产品详情
生物活性:
AN3661, a potent antimalarial lead compound, targets a Plasmodium falciparum cleavage and polyadenylation specificity factor homologue subunit 3 (PfCPSF3). AN3661 inhibits Plasmodium falciparum laboratory-adapted strains (mean IC50=32 nM), Ugandan field isolates (mean ex vivo IC50=64 nM), and murine P. berghei and P. falciparum infections.
体内研究:
AN3661 (50-200 mg.kg; p.o.; daily for 4 days) inhibits murine P. berghei infections with ED90 (4 days) 0.34 mg/kg.AN3661 is administered orally for 4 days, beginning on the third day of infection, the ED90 4 days after initiation of treatment is 0.57?mg/kg.Animal Model:P. berghei-infected mice (malaria model)
Dosage:50, 100, 200 mg/kg
Administration:Orally; daily for 4 days
Result:Rapidly controlled parasitemias, with an ED90 of 0.34?mg/kg. Daily dosages of 50?mg/kg and 100?mg/kg extended survival, and mice treated with 200?mg/kg per day demonstrated long-term cures.
体外研究:
AN3661 is active at nanomolar (IC50=20-56?nM) concentrations against P. falciparum laboratory strains known to be sensitive (3D7) or resistant (W2, Dd2, K1, HB3, FCR3 and TM90C2B), and AN3661 is similarly active in ex vivo studies of fresh Ugandan field isolates (mean ex vivo IC50=64?nM). AN3661 shows minimal cytotoxicity against mammalian cell lines, with the CC50 60.5?μM against Jurkat cells, and all other CC50 values greater than the highest concentrations tested (25?μM or above).AN3661 inhibits the stability of P. falciparum transcripts.