AN3661，一种有效的抗疟疾先导化合物，靶向恶性疟原虫的切割和多腺苷酸特异性因子同源物亚基 3 (PfCPSF3)。AN3661 可抑制恶性疟原虫实验室适应的菌株(平均 IC₅₀=32 nM)，Ugandan 野外分离株 (平均 IC₅₀=64 nM) 和小鼠 P. berghei 和 P. falciparum 的感染。

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 IC 50 =32 nM), Ugandan field isolates (mean ex vivo IC 50 =64 nM), and murine P. berghei and P. falciparum infections.

Solid

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. has not independently confirmed the accuracy of these methods. They are for reference only.

AN3661 (50-200 mg.kg; p.o.; daily for 4 days) inhibits murine P. berghei infections with ED 90 (4 days) 0.34 mg/kg.
AN3661 is administered orally for 4 days, beginning on the third day of infection, the ED 90 4 days after initiation of treatment is 0.57?mg/kg. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Sonoiki E, et al. A potent antimalarial benzoxaborole targets a Plasmodium falciparum cleavage and polyadenylation specificity factor homologue. Nat Commun. 2017;8:14574. Published 2017 Mar 6.

In Vitro: DMSO : 250 mg/mL (1213.59 mM; Need ultrasonic)配制储备液