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，Ugandan 野外分离株和小鼠 P. berghei 和 P. falciparum 的感染。
货号:ajcx29112
CAS:1268335-33-6
分子式:C10H11BO4
分子量：206
溶解度:DMSO: 250 mg/mL (1213.59 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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, Ugandan field isolates, and murine P. berghei and P. falciparum infections[1].

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)[1].AN3661 inhibits the stability of P. falciparum transcripts[1].

AN3661 (50-200 mg.kg; p.o.; daily for 4 days) inhibits murine P. berghei infections with ED90 (4 days) 0.34 mg/kg[1].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[1]. Animal Model: P. berghei-infected mice (malaria model)[1]

[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.