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139226-28-1

中文名稱 (5Z)-2-氨基-5-[(4-羥基-3,5-二叔丁基苯基)亞甲基]-1,3-噻唑-4-酮
英文名稱 (5Z)-2-Amino-5-[(4-hydroxy-3,5-ditert-butyl-phenyl)methylidene]-1,3-thiazol-4-one
CAS 139226-28-1
分子式 C18H24N2O2S
分子量 332.46
MOL 文件 139226-28-1.mol
更新日期 2023/03/20 15:41:17
139226-28-1 結(jié)構(gòu)式 139226-28-1 結(jié)構(gòu)式

基本信息

中文別名
達(dá)布非隆
達(dá)布飛龍
達(dá)布非龍,
5-((Z)-4-羥基-3,5-二叔丁基苯基亞甲基)-2-亞氨基-4-噻唑烷酮
(5Z)-2-氨基-5-[(4-羥基-3,5-二叔丁基苯基)亞甲基]-1,3-噻唑-4-酮
英文別名
CS-490
darbufelone
(Z)-2-AMino-5-(3,5-di-tert-butyl-4-hydroxybenzylidene)thiazol-4(5H)-one
5-((z)-3,5-di-tert-butyl-4-hydroxybenzylidene)-2-imino-4-thiazolidinone
(5Z)-2-amino-5-[(3,5-ditert-butyl-4-hydroxyphenyl)methylidene]-1,3-thiazol-4-one
(5z)-2-amino-5-[(4-hydroxy-3,5-ditert-butyl-phenyl)methylidene]-1,3-thiazol-4-one
4(5H)-Thiazolone, 2-amino-5-[[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]methylene]-, (5Z)-

物理化學(xué)性質(zhì)

沸點(diǎn)448.6±55.0 °C(Predicted)
密度1.18±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)9.98±0.50(Predicted)
形態(tài)Solid
顏色White to off-white
(5Z)-2-氨基-5-[(4-羥基-3,5-二叔丁基苯基)亞甲基]-1,3-噻唑-4-酮價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2024/01/25HY-101438(5Z)-2-氨基-5-[(4-羥基-3,5-二叔丁基苯基)亞甲基]-1,3-噻唑-4-酮
Darbufelone
139226-28-11mg2000元

常見問題列表

生物活性
Darbufelone 是細(xì)胞 PGF2α 和 LTB4 產(chǎn)生的雙重抑制劑。Darbufelone 有效抑制 PGHS-2 (IC50=0.19 μM),但對(duì) PGHS-1 效力要低得多 (IC50=20 μM)。
靶點(diǎn)

IC50: 0.19 μM (PGHS-2), 20 μM (PGHS-1)

體外研究

Darbufelone is a noncompetitive inhibitor of PGHS-2 (K i =10±5 μM). Darbufelone quenches the fluorescence of PGHS-2 at 325 nm (lambda(ex)=280 nm) with K d =0.98±0.03 μM.To test the putative anti-proliferative effect of Darbufelone, A549, H520 and H460 cell lines are used, which are established from three distinct pathological subtypes of NSCLC (adenocarcinoma, squamous and large cell lung cancer respectively). Increasing concentrations of Darbufelone, ranging from 5 to 60 μM, are tested for 72 h. The cell growth inhibition of these three cell lines gradually increases with higher drug concentration. The IC 50 of A549 and H520 are 20±3.6 and 21±1.8 μM, respectively, while the H460 has much lower IC 50 (15±2.7 μM).

體內(nèi)研究

Darbufelone is a dual inhibitor of cellular PGF2R and LTB4 production. Darbufelone is orally active and nonulcerogenic in animal models of inflammation and arthritis. When mice are treated with Darbufelone at dosage of 80 mg/kg/day, the tumor volumes decrease in a time-dependent manner. In contrast, lower dose of Darbufelone (20 or 40 mg/kg/day) dos not show any significant inhibition of tumor weight. At necropsy, the tumor weight in mice treated with Darbufelone (80 mg/kg/day) is reduced by 30.2% in comparison with control group.

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