894787-30-5
中文名称
(2R,4'R,8'AR)-1-[2-[4-[[2-(2,4-二氯苯氧基)乙酰基]氨基]苯基]乙酰基]四氢-6'-氧代螺[吡咯烷-2,7'(6'H)-[2H]吡咯并[2,1-B][1,3]噻嗪]-4'-甲酰胺
英文名称
ST 2825
CAS
894787-30-5
分子式
C27H28Cl2N4O5S
分子量
591.51
MOL 文件
894787-30-5.mol
894787-30-5 结构式
基本信息
中文别名
(2R,4'R,8'AR)-1-[2-[4-[[2-(2,4-二氯苯氧基)乙酰基]氨基]苯基]乙酰基]四氢-6'-氧代螺[吡咯烷-2,7'(6'H)-[2H]吡咯并[2,1-B][1,3]噻嗪]-4'-甲酰胺 英文别名
ST 2825ST 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
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)-
物理化学性质
沸点939.0±65.0 °C(Predicted)
密度1.51±0.1 g/cm3(Predicted)
溶解度溶于二甲基亚砜
酸度系数(pKa)12.86±0.70(Predicted)
形态固体
常见问题列表
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.