DDD107498 succinate (DDD-498 succinate) 是一种有效、可口服的抗疟疾 (antimalarial) 剂,具有良好的药代动力学特性和可接受的安全性。DDD107498 succinate 对于寄生虫多个生命周期阶段具有强大的抗疟活性,对P. falciparum3D7 的EC50值为 1 nM。DDD107498 succinate (DDD-498 succinate) 通过靶作用于eEF2/CaMKIII来抑制蛋白合成,对 WT-PfeEF2 的EC50值为 2 nM。
产品描述
DDD107498 succinate (DDD-498 succinate) is a potent and orally active antimalarial agent with good pharmacokinetic properties and an acceptable safety profile. DDD107498 succinate inhibits multiple life-cycle stages of the parasite with an EC 50 of 1 nM against P. falciparum 3D7. DDD107498 succinate inhibits protein synthesis by targeting eEF2/CaMKIII, with an EC 50 of 2 nM for WT- Pf eEF2 [1].
体外活性
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].
体内活性
DDD107498 shows an ED 90 of 0.57 mg/kg after a single oral dose in mice infected with the rodent parasite P. berghei [1].
Cas No.
2444781-71-7
分子式
C31H37FN4O6
分子量
580.65
别名
MMV121;DDD498;琥珀酸DDD107498;M 5717;DDD107498 succinate
储存和溶解度
DMSO:120 mg/mL (206.66 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years