Tranilast Sodium

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Tranilast Sodium

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

104931-56-8

包装与价格：

包装	价格(元)
10mg	电议
50mg	电议

产品名称

曲尼司特钠
MK-341 sodium
SB 252218 sodium

产品介绍

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。

生物活性

Tranilast sodium (MK-341 sodium) acts as an anti-atopic agent. Tranilast suppresses production ofprostaglandin D2(PGD2,IC₅₀= 0.1 mM). Tranilast sodium exhibits anti-inflammatory and immunomodulatory effects^[1]. Tranilast sodium antagonizesangiotensin IIand inhibits its biological effects in vascular smooth muscle cells^[2].

IC₅₀& Target

Angiotensin II

体外研究
(In Vitro)

Tranilast exhibits significant immunomodulatory activity inhibiting Endotoxin-induced prostaglandin E2 (PGE2; IC₅₀=~1-20 μM), thromboxane B2 (IC₅₀=~10-50 μM), (TGF-β1; IC₅₀=~100-200 μM), and IL-8 (IC₅₀=~100 μM) formation. A23187-induced monocyte leukotriene C4 or PGE2 formation is inhibited by Tranilast at IC₅₀s of 10-40 μM and 2-20 μM, respectively^[3].
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^[4].
Tranilast (12.5, 25, 50, 100 μg/mL; 72 hours) inhibits proliferation of HDMECs^[5].

Cell Proliferation Assay^[4]

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^[5]

Cell Line:	Human dermal microvascular endothelial cells (HDMECs)
Concentration:	12.5, 25, 50, 100 μg/mL
Incubation Time:	72 hours
Result:	IC₅₀value was 44.3 μg/mL (136 μM).

体内研究
(In Vivo)

Tranilast (300 mg/kg; administered orally twice a day for 3 days) dose-dependently suppresses angiogenesis in mice^[5].

Animal Model:	Nine-week-old male C57BL/6 mice^[5]
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 ED₅₀value and 95% confidence limits were 165 mg/kg and 162±169 mg/kg, respectively.

Clinical Trial

分子量

349.31

Formula

C₁₈H₁₆NNaO₅

CAS 号

104931-56-8

中文名称

曲尼司特钠

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.