Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DDD107498 (MMV121) (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 (MMV121) (DDD-498) 通过靶向 eEF2/CaMKIII 来抑制蛋白合成,对 WT-PfeEF2 的EC50值为 2 nM。
产品描述 | DDD107498 (MMV121) (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 (MMV121) inhibits protein synthesis by targeting eEF2/CaMKIII, with an EC 50 of 2 nM for WT- Pf eEF2 [1]. |
靶点活性 | P. falciparum (3D7):1 nM (EC50) |
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 | At a dose of 3 mg/kg, DDD107498 was fully curative with no sign of parasitaemia after 30 days [1]. |
别名 | M 5717, DDD498, MMV121 |
分子量 | 462.57 |
分子式 | C27H31FN4O2 |
CAS No. | 1469439-69-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 4.63 mg/mL (10 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1618 mL | 10.8092 mL | 21.6183 mL | 54.0459 mL |
5 mM | 0.4324 mL | 2.1618 mL | 4.3237 mL | 10.8092 mL | |
10 mM | 0.2162 mL | 1.0809 mL | 2.1618 mL | 5.4046 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
DDD107498 1469439-69-7 Microbiology/Virology Parasite M-5717 DDD-107498 protein Calmodulin-dependent kinases synthesis antimalarial stage eEF2 MMV 121 infection M 5717 Inhibitor CaMK DDD 498 multiple DDD498 Calmodulin-dependent protein kinases DDD-498 inhibit DDD 107498 MMV121 MMV-121 M5717 inhibitor