罗格列酮 T0334

Product Introduction
Bioactivity


英文名: Rosiglitazone

描述: Rosiglitazone (BRL49653) 是一种 PPARγ 激动剂、TRPC5 激活剂和 TRPM3 抑制剂，具有口服活性。Rosiglitazone 也是一种降糖剂，是噻唑烷二酮类胰岛素增敏剂。

细胞实验: Rosiglitazone is dissolved in DMSO and stored, and then diluted with appropriate medium before use[2]. Human neuroblastoma SH-SY5Y cells are maintained in Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% fetal bovine serum, 100 μg/mL Streptomycin and 100 U/mL Penicillin G. SH-SY5Y cells are transfected with the longest isoform of human tau (2N4R) tagged with GFP using lipofectamine. 24 hr after transfection, cells are treated with Rosiglitazone (10 μM, 50 μM) for 24 hr[2].

体外活性: 方法：人神经母细胞瘤细胞 SK-N-AS 和 SH-SY5Y 用 Rosiglitazone (0.1-20 μM) 处理 48 h，使用 MTS 检测细胞活力。结果：Rosiglitazone 显著降低 SK-N-AS 细胞活力，20 μM 处理的抑制率为 54%。Rosiglitazone 也能降低 SH-SY5Y 细胞活力，但 20 μM 处理组的降幅仅为 13%。[1]方法：小鼠单核巨噬细胞 RAW264.7 用 Rosiglitazone (1-25 μM) 处理 30 min，随后用 LPS (5 μg/mL) 刺激 24 h，使用 Griess reagent 检测 NO 释放，使用 PGE2 EIA kit 检测 PGE2 的产生。结果：Rosiglitazone 预处理显著阻断 LPS 诱导的 NO 释放和 PGE2 产生。[2]

体内活性: 方法：为研究对 NAFLD 模型中肝脏组织学和线粒体功能的影响，将 Rosiglitazone (1 mg/kg) 灌胃给药给 ob/ob C57BL/6J 小鼠，每天一次，持续十二周。结果：Rosiglitazone 治疗 ob/ob 小鼠不能逆转 NAFLD 的组织学损伤或提高 MRC 活性。相反，Rosiglitazone 降低复合物 I 的活性，增加氧化应激和肝脂肪变性。[3]方法：为研究对糖尿病神经病变 (DN) 发展的影响，将 Rosiglitazone (3 mg/kg) 口服给药给用 STZ 诱导糖尿病的 DBA/2J 小鼠，每天一次，持续二十四周。结果：Rosiglitazone 治疗不影响高血糖，但可以减少氧化应激，防止热痛觉减退的发展。[4]

存储条件: store at low temperaturePowder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: 1eq. HCl : 35.7 mg/mL (100 mM)
5% DMSO+95% Saline : 1.79 mg/mL (4.99 mM, suspension)
DMSO : 45 mg/mL (125.9 mM)


关键字: diabetic | PPAR | neuroprotection | senescence | PPARγ | Inhibitor | cancer | diabetes | Autophagy | Rosiglitazone | BRL-49653 | HCC | antihyperglycemic | TRP Channel | bladder | mellitus | Peroxisome proliferator-activated receptors | inhibit | BRL 49653 | carcinoma | smoke | Apoptosis | ovarian cancer | Transient receptor potential channels | hepatocellular | Ferroptosis

相关产品: (E)-Ferulic acid | FA16 | L-Glutamine | Piperlongumine | Nordihydroguaiaretic acid | Eprenetapopt | Anticancer agent 147 | Pioglitazone | Sorafenib | L-Glutamic acid

相关库: Drug Repurposing Compound Library | Drug-induced Liver Injury (DILI) Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Nuclear Receptor Compound Library | Traditional Chinese Medicine Monomer Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途