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Tranilast
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CAS NO:53902-12-8
包装与价格:
包装价格(元)
10 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
曲尼司特
MK 341
SB 252218
产品介绍
Tranilast 是一种抗过敏药物,可抑制炎症细胞释放脂质介质和细胞因子,抑制前列腺素 D2 (PGD2)产生,IC50为 0.1 mM。它拮抗血管紧张素 II 并抑制其在血管平滑肌细胞中的生物学作用,具有抗炎和免疫调节作用。

产品描述

Tranilast, an antiallergic drug, suppresses lipid mediator and cytokine release from inflammatory cells, therefore utilized in the treatment of allergic disorders.

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。

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].

Cas No.

53902-12-8

分子式

C18H17NO5

分子量

327.33

别名

曲尼司特;MK 341;SB 252218

储存和溶解度

DMSO:32.7 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years