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158089-95-3

中文名稱 158089-95-3
英文名稱 S-2474
CAS 158089-95-3
分子式 C20H31NO3S
分子量 365.53
MOL 文件 158089-95-3.mol
158089-95-3 結(jié)構(gòu)式 158089-95-3 結(jié)構(gòu)式

基本信息

中文別名
化合物 T16817
英文別名
S-2474
2,6-ditert-butyl-4-[(2-ethyl-1,1-dioxo-1,2-thiazolidin-5-ylidene)methyl]phenol
Phenol, 2,6-bis(1,1-dimethylethyl)-4-[(E)-(2-ethyl-1,1-dioxido-5-isothiazolidinylidene)methyl]-

物理化學(xué)性質(zhì)

熔點135-137 °C
沸點462.7±55.0 °C(Predicted)
密度1.129±0.06 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)11.28±0.50(Predicted)

常見問題列表

生物活性
S-2474 是 COX-2 和 5-lipoxygenase (5-LO) 的抑制劑,在人完整的細胞中,對 COX-2 和 COX-1 的 IC50 值分別為 11 nM 和 27 μM,為一種非甾體抗炎藥。
靶點

COX-2

11 nM (IC 50 )

COX-1

27 μM (IC 50 )

5-LO

體外研究

S-2474 is an inhibitor of COX-2 and 5-lipoxygenase, with IC 50 s of 11 nM and 27 μM for COX-2 and COX-1. S-2474 prevents neurons from Aβ-induced cell death significantly in a concentration-dependent manner (IC 50 =26±12?nM). S-2474 (10?μM) completely inhibits Aβ(25-35)-induced neuronal cell death. S-2474 also shows neuroprotective effects in the Aβ(1-40)-induced neuronal cell death. S-2474 inhibits the PGD2 generation in a concentration dependent manner (IC 50 =69.8±21.9?nM). S-2474 (10?μM) lowers the elevated level of PGD2 significantly and reduces radicals from Aβ(25-35)-treated neurons. S-2474 significantly prevents neurons from undergoing sPLA 2 -IIA-induced cell death. S-2474 completely ameliorates sPLA 2 -IIA-induced apoptotic features such as the condensation of chromatin and the fragmentation of DNA. Moreover, S-2474 significantly inhibits the sPLA 2 -IIA-induced generation of PGD2. S-2474 inhibits sPLA 2 -IIA-induced neuronal cell death in a concentration-dependent manner (IC 50 = 94 nM).

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