| 名稱 | 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. |
| 激酶實(shí)驗(yàn) | 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]. |
| 體外活性 | 在糖尿病大鼠的心臟中,Tranilast減少磷酸化Smad2, 能夠降低心臟纖維化. |
| 體內(nèi)活性 | 在瘢痕瘤和增生性瘢痕組織中, Tranilast（3-300 mM）通過抑制抑制轉(zhuǎn)化生長因子（TGF）-β1,從而抑制成纖維細(xì)胞的膠原合成,但它不抑制正常的皮膚成纖維細(xì)胞。 |
| 存儲條件 | 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.
|
| 關(guān)鍵字 | 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 |
| 相關(guān)產(chǎn)品 | Rutin | Azilsartan Methyl Ester | Sacubitril/Valsartan | Losartan | Captopril | Ramipril | Ethamsylate | Irbesartan | Ozagrel | Losartan potassium | Enalapril Maleate | Pranoprofen |
| 相關(guān)庫 | 抗癌上市藥物庫 | 經(jīng)典已知活性庫 | 已知活性化合物庫 | 清熱解毒中藥單體庫 | 臨床失敗化合物庫 | 抗衰老化合物庫 | GPCR靶點(diǎn)分子庫 | 膜蛋白靶向化合物庫 | 藥物功能重定位化合物庫 | 疼痛相關(guān)化合物庫 | 抗癌臨床化合物庫 | 抗癌藥物庫 |