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2123480-72-6

中文名称 UbcH5c-IN-6d
英文名称 UbcH5c-IN-6d
CAS 2123480-72-6
分子式 C22H21BrO3
分子量 413.3
MOL 文件 2123480-72-6.mol
2123480-72-6 结构式 2123480-72-6 结构式

基本信息

中文别名
化合物 T13242
英文别名
UbcH5c-IN-1
UbcH5c-IN-6d
UbcH5c IN 1,UbcH5cIN1,UbcH-5c-IN-1
Naphtho[1,2-b]furan-2(3H)-one, 8-[(2-bromophenyl)methoxy]-3a,4,5,9b-tetrahydro-6,9-dimethyl-3-methylene-, (3aS,9bR)-

物理化学性质

沸点559.8±50.0 °C(Predicted)
密度1.41±0.1 g/cm3(Predicted)
储存条件-20°C储存
溶解度溶于二甲基亚砜

常见问题列表

生物活性
UbcH5c-IN-1 (compound 6d) 是一种有效的、选择性的小分子泛素结合酶 UbcH5c 抑制剂,其与 E2 UbcH5c-IN-1 活性位点Cys85共价结合的 Kd 值为 283 nM,是开发新型类风湿性关节炎药物的先导化合物。
靶点

Kd: 283 nM (E2 UbcH5c).

体内研究

UbcH5c-IN-1 (compound 6d) (5 and 20 mg/kg, p.o., daily, 10-20 days) treatment in Freund’s adjuvant (CFA)-induced adjuvant arthritis (AA) rat model results in appreciable decreases in the arthritis index score and hind paw swelling rate compared with those of the vehicle-treated AA model control group.

Animal Model: Freund’s adjuvant (CFA)-induced adjuvant arthritis (AA) rat model.
Dosage: 5 and 20 mg/kg
Administration: Oral administration daily between day 10-20 postimmunization.
Result: Resulted in appreciable decreases in the arthritis index score and hind paw swelling rate compared with those of the vehicle-treated AA model control group.
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