甲磺酸達(dá)布非龍
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- CAS號:
- 139340-56-0
- 英文名:
- Darbufelone mesilate
- 英文別名:
- CI 1004;CI-1004 mesylate;DARBUFELONE MESILATE;Darbufelone (mesylate);Darbufelone mesylate (CI-1004 mesylate);(5Z)-2-Amino-5-[(3,5-ditert-butyl-4-hydroxyphenyl)methylidene]-1,3-thiazol-4-one methanesulfonate
- 中文名:
- 甲磺酸達(dá)布非龍
- 中文別名:
- 甲磺酸達(dá)布非隆;甲磺酸達(dá)布非龍;達(dá)布非龍甲磺酸鹽;化合物 T10960L;(5Z)-2-氨基-5-[(3,5-二叔丁基-4-羥基苯基)亞甲基]-1,3-噻唑-4-酮甲磺酸鹽
- CBNumber:
- CB71366591
- 分子式:
- C19H28N2O5S2
- 分子量:
- 428.56
- MOL File:
- 139340-56-0.mol
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甲磺酸達(dá)布非龍化學(xué)性質(zhì)
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儲存條件:
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4°C, protect from light
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溶解度:
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Soluble in DMSO
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形態(tài):
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Solid
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顏色:
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White to light yellow
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甲磺酸達(dá)布非龍性質(zhì)、用途與生產(chǎn)工藝
Darbufelone mesylate (CI-1004 mesylate) 雙重抑制細(xì)胞 PGF2α 和 LTB4 產(chǎn)生。Darbufelone 有效抑制 PGHS-2 (IC50=0.19 μM)，但對 PGHS-1 效力要低得多 (IC50=20 μM)。
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PGF
2α
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LTB
4
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PGHS-2
0.19 μM (IC
50
)
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PGHS-1
20 μM (IC
50
)
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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) .
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.
甲磺酸達(dá)布非龍
上下游產(chǎn)品信息
上游原料
下游產(chǎn)品
| 更新日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS編號 | 包裝 | 價(jià)格 |
|---|
| 2025/02/08 | HY-101438A | 甲磺酸達(dá)布非龍
Darbufelone mesylate | 139340-56-0 | 1 mg | 500元 |
| 2025/02/08 | HY-101438A | 甲磺酸達(dá)布非龍
Darbufelone mesylate | 139340-56-0 | 10 mM * 1 mLin DMSO | 1226元 |
139340-56-0, 甲磺酸達(dá)布非龍 相關(guān)搜索:
- 抑制劑
- C18H24N2O2SCH4O3S
- 達(dá)布非龍甲磺酸鹽
- 化合物 T10960L
- 甲磺酸達(dá)布非隆
- 甲磺酸達(dá)布非龍
- (5Z)-2-氨基-5-[(3,5-二叔丁基-4-羥基苯基)亞甲基]-1,3-噻唑-4-酮甲磺酸鹽
- 139340-56-0
- Darbufelone mesylate (CI-1004 mesylate)
- CI-1004 mesylate
- Darbufelone (mesylate)
- (5Z)-2-Amino-5-[(3,5-ditert-butyl-4-hydroxyphenyl)methylidene]-1,3-thiazol-4-one methanesulfonate
- DARBUFELONE MESILATE
- CI 1004