Tranilast(Synonyms: 曲尼司特; MK-341; SB 252218)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Tranilast (Synonyms: 曲尼司特; MK-341; SB 252218) 纯度: 99.46%

Tranilast (MK-341) 是一种抗变态反应剂。抑制前列腺素 D2 产生 (PGD2IC50=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。

Tranilast(Synonyms: 曲尼司特; MK-341;  SB 252218)

Tranilast Chemical Structure

CAS No. : 53902-12-8

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10 mM * 1 mL in DMSO ¥500 In-stock
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生物活性

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

IC50 & Target

PGD2

0.1 mM (IC50)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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 Viability Assay[5]

Cell Line: Human dermal microvascular endothelial cells (HDMECs)
Concentration: 12.5, 25, 50, 100 μg/mL
Incubation Time: 72 hours
Result: IC50 value 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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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 ED50 value and 95% confidence limits were 165 mg/kg and 162±169 mg/kg, respectively.

Clinical Trial

分子量

327.33

Formula

C18H17NO5

CAS 号

53902-12-8

中文名称

曲尼司特

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (152.75 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.0550 mL 15.2751 mL 30.5502 mL
5 mM 0.6110 mL 3.0550 mL 6.1100 mL
10 mM 0.3055 mL 1.5275 mL 3.0550 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 30 % SBE-β-CD

    Solubility: 5 mg/mL (15.28 mM); Suspended solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 1.5% CMC-Na/saline water

    Solubility: 4 mg/mL (12.22 mM); Suspended solution; Need ultrasonic

  • 3.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.64 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.64 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 4.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (7.64 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (7.64 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 5.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.64 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.64 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. K Ikai , et al. Inhibitory Effect of Tranilast on Prostaglandin D Synthetase. Biochem Pharmacol. 1989 Aug 15;38(16):2673-6.

    [2]. K Miyazawa , et al. Tranilast Antagonizes Angiotensin II and Inhibits Its Biological Effects in Vascular Smooth Muscle Cells. Atherosclerosis. 1996 Apr 5;121(2):167-73.

    [3]. E A Capper, et al. Modulation of Human Monocyte Activities by Tranilast, SB 252218, a Compound Demonstrating Efficacy in Restenosis. J Pharmacol Exp Ther. 2000 Dec;295(3):1061-9.

    [4]. Sara Darakhshan, et al. Tranilast Enhances the Anti-Tumor Effects of Tamoxifen on Human Breast Cancer Cells in Vitro. J Biomed Sci. 2013 Oct 21;20(1):76.

    [5]. M Isaji , et al. Tranilast Inhibits the Proliferation, Chemotaxis and Tube Formation of Human Microvascular Endothelial Cells in Vitro and Angiogenesis in Vivo. Br J Pharmacol. 1997 Nov;122(6):1061-6.

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