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].

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.

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.

327.33

C₁₈H₁₇NO₅

53902-12-8

曲尼司特

Room temperature in continental US; may vary elsewhere.

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

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。

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。

• [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.