192755-52-5
中文名称
化合物 T16570
英文名称
(3S,11S)-N-[(2R,3S)-2-ethoxy-5-oxo-oxolan-3-yl]-3-(isoquinoline-1-carbonylamino)-2,6-dioxo-1,7-diazabicyclo[5.4.0]undecane-11-carboxamide
CAS
192755-52-5
分子式
C26H29N5O7
分子量
523.54
MOL 文件
192755-52-5.mol
192755-52-5 结构式
基本信息
中文别名
化合物 T16570 英文别名
VX-740HMR 3480
Pralnacasan
(3S,11S)-N-[(2R,3S)-2-ethoxy-5-oxo-oxolan-3-yl]-3-(isoquinoline-1-carbonylamino)-2,6-dioxo-1,7-diazabicyclo[5.4.0]undecane-11-carboxamide
(1S,9S)-N-[(2R,3S)-2-Ethoxy-5-oxotetrahydro-3-furanyl]-9-[(1-isoquinolinylcarbonyl)amino]-6,10-dioxooctahydro-6H-pyridazino[1,2-a][1,2]diazepine-1-carboxamide
6H-Pyridazino[1,2-a][1,2]diazepine-1-carboxamide, N-[(2R,3S)-2-ethoxytetrahydro-5-oxo-3-furanyl]octahydro-9-[(1-isoquinolinylcarbonyl)amino]-6,10-dioxo-, (1S,9S)-
常见问题列表
生物活性
Pralnacasan (VX-740) 是一种有效的，选择性的，非肽型，具有口服活性白介素 1β 转化酶 (ICE, caspase 1) 抑制剂，Ki 为 1.4 nM。Pralnacasan 抑制促炎细胞因子 IL-18，IL-1β 和 IFN-γ。Pralnacasan 有潜力用于骨关节炎和类风湿关节炎的研究。靶点
|
Interleukin-1β converting enzyme 1.4 nM (Ki) |
体内研究
Pralnacasan (0 -50 mg/kg; oral gavage; twice a day; for 6 weeks; female Balb/c mice) treatment reduces joint damage. Pralnacasan treatment does not appear to affect the weight of the animals.
| Animal Model: | Female Balb/c mice induced with collagenase |
| Dosage: | 0 mg/kg, 12.5 mg/kg, 25 mg/kg and 50 mg/kg |
| Administration: | Oral gavage; twice a day; for 6 weeks |
| Result: | Significantly ameliorated the histopathological damage of the medial knee joint compartments. |