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104931-56-8

中文名称 104931-56-8
英文名称 Tranilast (SodiuM)
CAS 104931-56-8
分子式 C18H16NNaO5
分子量 349.313
MOL 文件 104931-56-8.mol
104931-56-8 结构式 104931-56-8 结构式

基本信息

中文别名
曲尼司特钠
英文别名
Tranilast (SodiuM)

物理化学性质

储存条件-20°C储存
溶解度溶于二甲基亚砜
形态粉末

安全数据

危险性符号(GHS)
GHS07
警示词警告
危险性描述H302

常见问题列表

生物活性
Tranilast sodium (MK-341 sodium) 是一种抗变态反应剂。抑制前列腺素 D2 产生 (PGD2,IC50=0.1 mM)。具有抗炎和免疫调节作用。Tranilast sodium 拮抗血管紧张素 II (angiotensin II) 并抑制其在血管平滑肌细胞中的生物学作用。
靶点

PGD 2

0.1 mM (IC 50 )

Angiotensin II

体外研究

Tranilast exhibits significant immunomodulatory activity inhibiting Endotoxin-induced prostaglandin E2 (PGE2; IC 50 =~1-20 μM), thromboxane B2 (IC 50 =~10-50 μM), (TGF-β1; IC 50 =~100-200 μM), and IL-8 (IC 50 =~100 μM) formation. A23187-induced monocyte leukotriene C4 or PGE2 formation is inhibited by Tranilast at IC 50 s of 10-40 μM and 2-20 μM, respectively.
Tranilast (10-200 μM) exhibits the anti-proliferative effect in a dose-dependent manner in both MCF-7 and MDA-MB-231 cell lines. Tranilast also (10-200μM) enhances the anti-tumor effects of Tamoxifen (1-20 μM) on human breast cancer cells in vitro.
Tranilast (12.5, 25, 50, 100 μg/mL; 72 hours) inhibits proliferation of HDMECs.

Cell Proliferation Assay

Cell Line: MCF-7 and MDA-MB-231 cells
Concentration: 10, 20, 50, 100, and 200 μM
Incubation Time: 48 hours
Result: Anti-proliferative effect in a dose-dependent manner in both cell lines.

Cell Proliferation Assay

Cell Line: Human dermal microvascular endothelial cells (HDMECs)
Concentration: 12.5, 25, 50, 100 μg/mL
Incubation Time: 72 hours
Result: IC 50 value was 44.3 μg/mL (136 μM).
体内研究

Tranilast (300 mg/kg; administered orally twice a day for 3 days) dose-dependently suppresses angiogenesis in mice.

Animal Model: Nine-week-old male C57BL/6 mice
Dosage: 300 mg/kg
Administration: Administered orally twice a day for 3 days
Result: Suppressed the VEGF-induced angiogenesis in matrigel; 58% of significant suppression was observed at a dose of 300 mg/kg.
The ED 50 value and 95% confidence limits were 165 mg/kg and 162±169 mg/kg, respectively.
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