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894787-30-5

中文名稱(chēng) (2R,4'R,8'AR)-1-[2-[4-[[2-(2,4-二氯苯氧基)乙?;鵠氨基]苯基]乙酰基]四氫-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
英文名稱(chēng) 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 結(jié)構(gòu)式 894787-30-5 結(jié)構(gòu)式

基本信息

中文別名
(2R,4'R,8'AR)-1-[2-[4-[[2-(2,4-二氯苯氧基)乙?;鵠氨基]苯基]乙?;鵠四氫-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
英文別名
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
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)-
所屬類(lèi)別
生物化工:激動(dòng)劑抑制劑

物理化學(xué)性質(zhì)

沸點(diǎn)939.0±65.0 °C(Predicted)
密度1.51±0.1 g/cm3(Predicted)
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)12.86±0.70(Predicted)
形態(tài)固體
顏色White to off-white

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302-H315-H319-H335
防范說(shuō)明P261-P305+P351+P338

常見(jiàn)問(wèn)題列表

生物活性
ST 2825 是一種特異的 MyD88 二聚化抑制劑。ST 2825 干擾 MyD88 對(duì) IRAK1 和 IRAK4 的募集,抑制 IL-1β 介導(dǎo)的 NF-κB 轉(zhuǎn)錄活性。
靶點(diǎn)

MyD88

體外研究

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.

體內(nèi)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.

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