PT4 是一种抗皮肤利什曼病 (CL) 的化合物。PT4 对两种Leishmania均有效，对L. amazonensis和L. braziliensis的 IC50分别为 125.18 和 233.18 μM。PT4 降低线粒体膜电位且提高活性氧产生，导致寄生虫死亡。PT4 具有有效的体内抗炎活性。

PT4 is a therapeutic agent against Cutaneous leishmaniasis (CL). PT4 is effective against both species of Leishmania, with IC 50 s of 125.18 and 233.18 μM for L. amazonensis and L. braziliensis, respectively. PT4 decreases of mitochondrial membrane potential and increases production of reactive oxygen species, which leads to parasite death. PT4 has a potent in vivo anti-inflammatory activity [1].

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.

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

1280738-47-7

C18H14N4O2

318.33

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years