| 名称 | Tranilast |
| 描述 | Tranilast (SB 252218), an antiallergic drug, suppresses lipid mediator and cytokine release from inflammatory cells, therefore utilized in the treatment of allergic disorders. |
| 激酶实验 | His-tagged human Mps1Cat encoding amino acids 510-857 is generated. For kinase assays, 500 ng is added to buffer (25 mM Tris-HCl, pH 7.4, 100 mM NaCl, 50 μg/mL BSA, 0.1 mM EGTA, 0.1% β-mercaptoethanol, 10 mM MgCl2, and 0.5 μg/mL myelin basic protein), AZ3146, and 100 μM γ-[32P]ATP (2 μCi/assay). Reactions are incubated at 30°C for 20 min, spotted onto P81 paper, washed in 0.5% phosphoric acid, and immersed in acetone. Phosphate incorporation is determined by scintillation counting. For immunoprecipitation kinase assays, HeLa cells are treated with nocodazole for 14 h, mitotic cells isolated, washed in PBS, and lysed for 30 min in 50 mM Tris-HCl, pH 7.4, 100 mM NaCl, 0.5% NP-40, 5 mM EDTA, 5 mM EGTA, 40 mM β-glycerophosphate, 0.2 mM PMSF, 1 mM DTT, 1 mM sodium orthovanadate, 20 mM sodium fluoride, 1 μM okadaic acid, and complete EDTA-free protease inhibitor cocktail. Full-length Mps1 is immunoprecipitated. Purified complexes are washed with lysis buffer containing 100 mM NaCl and assayed as described for the recombinant protein. To quantify 32P incorporation, reactions are stopped with SDS sample buffer and separated by SDS-PAGE followed by phosphorimaging. The plate is analyzed using a phosphorimager using AIDA software. To assess the specificity of AZ3146, a single-point screen is carried using kinase profiling service. 50 kinases are selected and assayed with 1 μM AZ3146[1]. |
| 体外活性 | 在糖尿病大鼠的心脏中,Tranilast减少磷酸化Smad2, 能够降低心脏纤维化. |
| 体内活性 | 在瘢痕瘤和增生性瘢痕组织中, Tranilast（3-300 mM）通过抑制抑制转化生长因子（TGF）-β1,从而抑制成纤维细胞的胶原合成,但它不抑制正常的皮肤成纤维细胞。 |
| 存储条件 | keep away from direct sunlight,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 50 mg/mL (152.75 mM), Sonication is recommended.
|
| 关键字 | vascular | tube | Tranilast | SB-252218 | SB252218 | ProstaglandinReceptor | Prostaglandin Receptor | prostaglandin | proliferation | MK-341 | MK341 | microvascular | Inhibitor | inhibit | growth | factor | endothelial | chemotaxis | anti-atopic | Angiotensin Receptor | Angiogenesis |
| 相关产品 | Rutin | Azilsartan Methyl Ester | Sacubitril/Valsartan | Losartan | Captopril | Ramipril | Ethamsylate | Irbesartan | Ozagrel | Losartan potassium | Enalapril Maleate | Pranoprofen |
| 相关库 | 抗癌上市药物库 | 经典已知活性库 | 已知活性化合物库 | 清热解毒中药单体库 | 临床失败化合物库 | 抗衰老化合物库 | GPCR靶点分子库 | 膜蛋白靶向化合物库 | 药物功能重定位化合物库 | 疼痛相关化合物库 | 抗癌临床化合物库 | 抗癌药物库 |