- 英文名称
- ST 2825
- 分子式
- C27H28Cl2N4O5S
- 分子量
- 591.51
- 中文别名
- 化合物 T16937; (2R,4'R,8A'R)-1-(2-(4-(2-(2,4-二氯苯氧基)乙酰氨基)苯基)乙酰基)-6'-氧代六氢螺[吡咯烷-2,7'-吡咯并[2,1-B][1,3]噻嗪]-4'-甲酰胺; 化合物 ST 2825; ST-2825; ST2825; (2R,4'R,8'aR)-1-[2-[4-[[2-(2,4-Dichlorophenoxy)acetyl]amino]phenyl]acetyl]tetrahydro-6'-oxospiro[pyrrolidine-2,7'(6'H)-[2H]pyrrolo[2,1-b][1,3]thiazine]-4'-carboxamide; ST2825; Spiro[pyrrolidine-2,7'(6'H)-[2H]pyrrolo[2,1-b][1,3]thiazine]-4'-carboxamide, 1-[2-[4-[[2-(2,4-dichlorophenoxy)acetyl]amino]phenyl]acetyl]tetrahydro-6'-oxo-, (2R,4'R,8'aR)-; (2R,4'R,8a'R)-1-(2-(4-(2-(2,4-Dichlorophenoxy)acetamido)phenyl)acetyl)-6'-oxotetrahydro-2'H,6'H-spiro[pyrrolidine-2,7'-pyrrolo[2,1-b][1,3]thiazine]-4'-carboxamide
- 用途
- - 生物活性
ST 2825 是一种特异的 MyD88 二聚化抑制剂。ST 2825 干扰 MyD88 对 IRAK1 和 IRAK4 的募集，抑制 IL-1β 介导的 NF-κB 转录活性。
- 靶点
MyD88
- 体外研究
ST2825 blocks IL-1R/TLR signaling by interfering with MyD88 homodimerization. ST2825 inhibits this interaction in a concentration-dependent manner with ~40% inhibition of dimerization at 5 μM ST2825 and 80% inhibition at 10 μM ST2825.
- 体内研究
ST2825 dose-dependently inhibits IL-1β-induced production of IL-6 in treated mice after oral administration. The animals are administered orally with the appropriate vehicles or ST2825 at doses ranging from 50 to 200 mg/kg, 5 min prior to i.p. injection with 20 μg/kg IL-1β. ST2825 exertes a significant inhibition of IL-1β-stimulated production of IL-6 at 100 and 200 mg/kg.
