DDD107498 (DDD-498) 是一种有效口服活性的抗疟疾 (antimalarial) 剂，可抑制寄生虫生命周期的多个阶段，对P. falciparum3D7 的EC50值为 1 nM。DDD107498 (DDD-498) 通过靶向eEF2/CaMKIII来抑制蛋白合成，对 WT-PfeEF2 的EC50值为 2 nM。

DDD107498 (DDD-498) is a potent and orally active antimalarial agent that inhibits multiple life-cycle stages of the parasite with an EC 50 of 1 nM against P. falciparum 3D7. DDD107498 inhibits protein synthesis by targeting eEF2/CaMKIII, with an EC 50 of 2 nM for WT- Pf eEF2 [1].

DDD107498 showed excellent activity against 3D7 parasites: EC50 =1.0 nM; EC90 = 2.4 nM; EC99 = 5.9 nM. It was also almost equally active against a number of drug-resistant strains. Furthermore, DDD107498 was more potent than artesunate in ex vivo assays against a range of clinical isolates of both P. falciparum (median EC50 = 0.81) and P. vivax (median EC50 = 0.51 nM) [1].

At a dose of 3 mg/kg, DDD107498 was fully curative with no sign of parasitaemia after 30 days [1].

1469439-69-7

C27H31FN4O2

462.56

MMV121;DDD498;M 5717

DMSO:10 mM
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In solvent: -80°C for 2 years