Tranilast (MK-341) 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 (MK-341) 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]. |
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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 Viability 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). |
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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. |
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| 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 |
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| 溶解性数据 | In Vitro: DMSO : 50 mg/mL(152.75 mM;Need ultrasonic) 配制储备液 | 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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。 4. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 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本网站选购。
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