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Sulindac sulfone

Sulindac sulfone用途

依舒林是一种非甾体抗炎药舒林酸的非活性代谢产物。依舒林在体外抑制醛糖还原酶,IC50为367 nM,可能有助于舒林酸对2型糖尿病并发症的有益药理作用[2]。

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Sulindac sulfone名称

[ CAS 号 ]:
59864-04-9

[ 中文名 ]:
磺基舒林

[ 英文名 ]:
Exisulind

[中文别名 ]:

舒林酸砜

[英文别名 ]:

MFCD01317811
Exisulind
Sulindac Sulfone

Sulindac sulfone生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 醛糖还原酶

研究领域 >> 代谢疾病

[参考文献]

[1]. Kitamura S, Tatsumi K. In vitro metabolism of sulindac and sulindac sulfide: enzymatic formation of sulfoxide and sulfone. Jpn J Pharmacol. 1982 Oct;32(5):833-8.

[2]. Zheng X, et al. The molecular basis for inhibition of sulindac and its metabolites towards human aldose reductase. FEBS Lett. 2012 Jan 2;586(1):55-9.

Sulindac sulfone物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
601.9±55.0 °C at 760 mmHg

[ 分子式 ]:
C₂₀H₁₇FO₄S

[ 分子量 ]:
372.41

[ 闪点 ]:
317.8±31.5 °C

[ 精确质量 ]:
372.083160

[ PSA ]:
79.82000

[ LogP ]:
3.54

[ 蒸汽压 ]:
0.0±1.8 mmHg at 25°C

[ 折射率 ]:
1.620

[ 储存条件 ]:
-20°C，密闭，干燥

Sulindac sulfone安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

Sulindac sulfone文献

Exisulind: Aptosyn, FGN 1, Prevatac, sulindac sulfone.

Drugs R. D. 5(4) , 220-6, (2004)

Exisulind [Aptosyn trade mark, FGN 1 trade mark, Prevatac trade mark, sulindac sulfone], the sulfone derivative of sulindac, is the lead compound in a series of selective apoptotic antineoplastic drug...

Sulindac sulfide, but not sulindac sulfone, inhibits colorectal cancer growth.

Neoplasia 1(2) , 170-6, (1999)

Sulindac sulfide, a metabolite of the nonsteroidal antiinflammatory drug (NSAID) sulindac sulfoxide, is effective at reducing tumor burden in both familial adenomatous polyposis patients and in animal...

Sulindac sulfone inhibits K-ras-dependent cyclooxygenase-2 expression in human colon cancer cells.

Cancer Res. 60(23) , 6607-10, (2000)

Both the sulfide and sulfone metabolites of sulindac, a nonsteroidal anti-inflammatory drug, display anticarcinogenic effects in experimental models. Sulindac sulfide inhibits cyclooxygenase (COX) enz...

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