Bioactivity | Antitrypanosomal agent 15 (compound 26) is an orally active, brain-penetrant, selective inhibitor against Trypanosoma cruzi proteasome, with an pIC50 of 7.4 and cruzi and human proteasome, respectively. Antitrypanosomal agent 15 has favorable ADME properties and can be used for Chagas disease study[1]. |
Invitro | Antitrypanosomal agent 15 (compound 26) 对T. cruzi amastigotes和宿主 VERO 细胞的pEC50 分别为 6.1 和 4.4,外排比为 1.8,FaSSIF (空腹模拟肠液溶解度) 为 339 μM[1]。 0 --> Antitrypanosomal agent 15 相关抗体: |
In Vivo | Antitrypanosomal agent 15 (compound 26) (50 mg/kg, 每日两次, 20 天, 口服) 显示出良好的溶解性和渗透性,但对慢性恰加斯病小鼠模型无作用[1]。 Animal Model: |
Name | Antitrypanosomal agent 15 |
Formula | C21H19FN4O4 |
Molar Mass | 410.40 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Thomas MG, et al. Structure-Guided Design and Synthesis of a Pyridazinone Series of Trypanosoma cruzi Proteasome Inhibitors. J Med Chem. 2023;66(15):10413-10431. |