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49627-27-2

中文名稱 SULINDAC
英文名稱 SULINDAC SULFIDE
CAS 49627-27-2
分子式 C20H17FO2S
分子量 340.41
MOL 文件 49627-27-2.mol
更新日期 2025/04/27 21:59:50
49627-27-2 結(jié)構(gòu)式 49627-27-2 結(jié)構(gòu)式

基本信息

中文別名
舒林酸硫醚
舒林酸相關化合物C(USP)
英文別名
Einecs 256-403-9
SULINDAC SULPHIDE
(Z)-Sulindac sulfide
cis-Sulindac sulfide
Sulindac EP Impurity C (Sulindac Sulfide)
Sulindac Impurity 3(Sulindac EP Impurity C)
(Z)-5-FLUORO-2-METHYL-1-[P-(METHYLTHIO)BENZYLIDENE]INDENE-3-ACETIC ACID
(Z)-5-FLUORO-2-METHYL-1-(4-METHYLTHIOBENZYLIDENE)-1H-INDEN-3-YLACETIC ACID
5-Fluoro-2-methyl-1-[(Z)-[4-(methylthio)phenyl]methylene]-1H-indene-3-acetic acid
(Z)-5-fluoro-2-methyl-1-[[4-(methylthio)phenyl]methylene]-1H-indene-3-acetic acid
所屬類別
醫(yī)藥中間體:雜環(huán)化合物

物理化學性質(zhì)

熔點189-191°C
儲存條件-20°C冷凍
溶解度DMSO: >22 mg/mL
形態(tài)solid
顏色yellow

安全數(shù)據(jù)

危險品標志Xn
危險類別碼22-42/43-63
WGK Germany3
海關編碼2930902000

圖譜信息

常見問題列表

生物活性
Sulindac sulfide 是 γ-secretase 的一個非競爭性抑制劑,其對 γ42-secretase 的 IC50 值為 20.2 μM。
靶點

IC50: 20.2 μM (γ 42 -secretase).

體外研究

Treatment with 100 μM of Sulindac sulfide (SSide) causes cell death presumably by inducing apoptosis, resulting in marked decrease in Aβgeneration as well as in total protein expression. The IC 50 value for Aβ42 secretion of Sulindac sulfide is 30.6±2.8 μM. SSone and naproxen have no effect either on Aβ40 or Aβ42 secretion as well as on Notch cleavage up to 100 μM. It is observed that an inhibition of γ 42 -secretase activity by Sulindac sulfide in a dose-dependent manner. The IC 50 value of SSide for inhibiting γ 42 -secretase activity in vitro is 20.2±2.6 μM. A decrease is found in slope by the increase of the concentration of SSide in the plot of rate against the enzyme concentration, suggesting that Sulindac sulfide is not an irreversible or pseudo-irreversible inhibitor. Moreover, when the dialyzed solubilizedγ-secretase fraction is pretreated with Sulindac sulfide against CHAPSO buffer without Sulindac sulfide, γ-secretase activity is almost totally recovered. From these data, it is strongly suggested that the genuine molecular target of Sulindac sulfide is the γ-secretase complex and that Sulindac sulfide works as a reversible γ-secretase inhibitor.

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