Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PT4 可治疗皮肤利什曼病 (CL) ,它通过降低线粒体膜电位并增加活性氧的产生,从而寄生虫死亡。PT4 对两种利什曼原虫均产生效果,其对L. amazonensis 和L. braziliensis 的 IC50值分别为 125.18 和 233.18 μM。PT4 同时在体内具有有效的抗炎活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 10,600 | 6-8周 | ||
50 mg | ¥ 13,800 | 6-8周 | ||
100 mg | ¥ 17,500 | 6-8周 |
产品描述 | PT4 is a treatment agent for Cutaneous leishmaniasis (CL). PT4 decreases of mitochondrial membrane potential and increases reactive oxygen species production, therefore leads to parasite death. PT4 is effective against both species of Leishmania. The IC50 values of PT4 against L. amazonensis and L. braziliensis are 125.18 and 233.18 μM , respectively. PT4 also shows potent anti-inflammatory activity in vivo [1]. |
体外活性 | PT4 (0-1256.5 μM, 48 hours) can inhibit mammalian cells viability [1]. PT4 (314.1-19.6 μM, 48 hours) inhibits the growth of promastigote and amastigote of L. amazonensis and L. braziliensis promastigotes [1]. PT4 causes depolarization of the mitochondrial membrane of L. amazonensis and L. braziliensis promastigotes and increasing ROS in mitochondria [1]. Cell Cytotoxicity Assay [1] Cell Line: Balb/c mice peritoneal exudate (mPEC), J774A.1 macrophages, Fibroblasts Concentration: 0-1256.5 μM Incubation Time: 48 hours Result: Inhibited mPEC, J774A.1 and fibroblasts with CC 50 value of 981.37 μM, 521.47 μM and 895.17 μM, respectively. Cell Proliferation Assay [1] Cell Line: L. amazonensis, L. braziliensis promastigotes Concentration: 314.1-19.6 μM Incubation Time: 48 hours Result: Inhibited promastigote of L. amazonensis and L. braziliensis promastigotes with IC 50 value of 70.46 μM and 181.73 μM, respectively. Inhibited amastigote of them with IC 50 value of 125.18 μM and 233.18 μM, respectively. |
体内活性 | The pharmacokinetic and toxicological parameters of PT4 Parameter HBA (≤10) 4 HBD (≤5) 0 LogP (≤5) 2.23 MW (≤500) g/mol 318.33 n-ROTB (≤10) 4 TPSA (A2) 68.09 BBB Yes GIA High P-GP substrate No Skin permeability (cm/s) -6.85 CYP450 2C9 inhibitor Yes CYP450 2D6 inhibitor No CYP450 2C19 inhibitor Yes CYP450 3A4 inhibitor No CYP450 1A2 inhibitor Yes Total Clearance (log ml/min/kg) 0.117 Renal OCT2 substrate No LD50 (mg/Kg) 4700 |
分子量 | 318.33 |
分子式 | C18H14N4O2 |
CAS No. | 1280738-47-7 |
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。
PT4 1280738-47-7 Inhibitor inhibitor inhibit