货号:A675778
同义名:
MK-341; SB 252218
Tranilast能够拮抗血管紧张素II,并作为抗过敏药物。它对NLRP3炎症小体具有抑制作用,但对NLRC4或AIM2炎症小体无效。Tranilast抑制了内源性NLRP3-ASC相互作用,但不影响NLRP3-NEK7相互作用,提示其可能直接靶向NLRP3。
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免费溶解
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]. |
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 << |
[1]Suzawa H, et al. Jpn J Pharmacol, 1992, 60(2), 91-96.
计算器 | ||||
存储液制备 | ![]() |
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 |
CAS号 | 53902-12-8 |
分子式 | C18H17NO5 |
分子量 | 327.33 |
SMILES Code | O=C(O)C1=CC=CC=C1NC(/C=C/C2=CC=C(OC)C(OC)=C2)=O |
MDL No. | MFCD00864787 |
别名 | MK-341; SB 252218; N-5'; N-(3',4'-Dimethyoxycinnamoyl) Anthranilic Acid; 3,4-DAA |
运输 | 蓝冰 |
InChI Key | NZHGWWWHIYHZNX-CSKARUKUSA-N |
Pubchem ID | 5282230 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place, inert atmosphere, room temperature |
溶解方案 |
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 以下溶解方案都请先按照体外实验的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
|
动物实验配方 |
PO 10% DMSO + 30% PEG400 + 2% tween 80 +58% H2O 5 mg/mL clear |