Tranilast
产品说明书
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同义名 : | MK-341; SB 252218; N-5'; N-(3',4'-Dimethyoxycinnamoyl) Anthranilic Acid; 3,4-DAA |
| CAS号 : | 53902-12-8 | |
| 货号 : | A675778 | |
| 分子式 : | C18H17NO5 | |
| 纯度 : | 99% | |
| 分子量 : | 327.33 | |
| MDL号 : | MFCD00864787 | |
| 存储条件： |
Pure form Keep in dark place, inert atmosphere, room temperature In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 50 mg/mL(152.75 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
PO 10% DMSO + 30% PEG400 + 2% tween 80 +58% H2O 5 mg/mL clear |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Tranilast is an orally bioavailable anti-allergic agent. Tranilast is also an inhibitor of EMT (epithelial-mesenchymal transition) and attenuated the expression of mesenchymal markers and angiogenesis-related genes in NF1-mutated (Neurofibromatosis type 1) sNF96.2 cells and in neurofibroma cells from NF1 patients[3]. Tranilast inhibited proliferation of HOS, 143B, U2OS and MG-63 osteosarcoma cells in a dose-dependent manner, as well as enhancing the effects of cisplatin and doxorubicin. The average combination index at effect levels for tranilast in combination with cisplatin was 0.57 in HOS, 0.4 in 143B, 0.39 in U2OS and 0.51 in MG-63 cells[4]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT00818805 | Allergic Conjunctivitis | Phase 4 | Completed | - | - |
| NCT01109121 | Moderate to Severe Gout ... 展开 >> Hyperuricemia 收起 << | Phase 2 | Completed | - | - |
| NCT01052987 | Gout Hyperuri... 展开 >>cemia 收起 << | Phase 2 | Completed | - | United States, Hawaii ... 展开 >> Nuon Investigative Site Honolulu, Hawaii, United States United States, Indiana Nuon Investigative Site Evansville, Indiana, United States United States, Texas Nuon Investigative Site Dallas, Texas, United States 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
3.06mL 0.61mL 0.31mL |
15.28mL 3.06mL 1.53mL |
30.55mL 6.11mL 3.06mL |
| 参考文献 |
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[1]Suzawa H, et al. Jpn J Pharmacol, 1992, 60(2), 91-96. |