化合物 PT4 T60836

Product Introduction
Bioactivity


英文名: PT4

描述: 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。

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

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途