Powder: -20°C for 3 years | In solvent: -80°C for 1 year
LXE408 is an orally active, kinetoplastid-selective proteasome inhibitor, exhibiting non-competitive inhibitory effects. It demonstrates an IC50 of 0.04 μM for L. donovani proteasome and an EC50 of 0.04 μM for L. donovani. Moreover, LXE408 shows limited ability to traverse the blood-brain barrier. Hence, LXE408 holds promise for advancing research in the field of visceral leishmaniasis (VL).
产品描述 | LXE408 is an orally active, kinetoplastid-selective proteasome inhibitor, exhibiting non-competitive inhibitory effects. It demonstrates an IC50 of 0.04 μM for L. donovani proteasome and an EC50 of 0.04 μM for L. donovani. Moreover, LXE408 shows limited ability to traverse the blood-brain barrier. Hence, LXE408 holds promise for advancing research in the field of visceral leishmaniasis (VL). |
体外活性 | LXE408 (compound 1) can occupy the pocket as a ternary complex with the proteasome. LXE408 shows no inhibition of the hERG channel (IC 50 >30 μM) in a manual patch clamp assay. LXE408 has a low propensity to cross the blood brain barrier (brain/plasma AUC ratio=0.03 in mice)[1]. |
体内活性 | LXE408 (compound 1; 0.3-10 mg/kg; PO; twice daily for 8 days) potently reduces the parasite burden in the liver in a dose-dependent manner[1]. LXE408 (1, 3, 10, 20 mg/kg; p.o.; b.i.d.; for 10 days) effects robust healing of parasite-induced skin lesions at the base of the tail in BALB/c mice infected with L. major[1]. LXE408 (5 mg/kg IV and 20 mg/kg PO) has a T 1/2 of 3.3 hours for mouse. LXE408 (3 mg/kg IV and 10 mg/kg PO) has a T 1/2 of 3.8 hours, a CL of 2.1 mL/min?kg, and a V ss of 0.53 L/kg for male Sprague-Dawley rat[1]. LXE408 (0.3 mg/kg IV and 1.0 mg/kg PO) has a T 1/2 of 3.8 hours for male beagle dog. LXE408 (0.3 mg/kg IV and 10 mg/kg PO) has a T 1/2 of 9.7 hours for male cynomolgus monkey[1]. Animal Model: Female BALB/c mice (6-8 weeks old) infected with L. donovani[1]Dosage: 0.3, 1, 3, 10 mg/kg Administration: PO; twice daily for 8 days Result: Led to a 95% and >99.84% reduction of parasite burden in the liver at 1 mg/kg and 10 mg/kg. Animal Model: Balb/C mice[1]Dosage: 5 mg/kg IV and 20 mg/kg PO (Pharmacokinetic Analysis) Administration: IV or PO Result: Had a T 1/2 of 3.3 hours, a CL of 2.3 mL/min?kg, and a V ss of 0.63 L/kg for mouse. |
别名 | LXE408 |
分子量 | 443.442 |
分子式 | C23H18FN7O2 |
CAS No. | 1799330-15-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
LXE408 1799330-15-6 LXE-408 LXE 408 Inhibitor inhibitor inhibit