Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Rosiglitazone (BRL 49653) potassium is a potent and selective PPARγ agonist (EC 50: 60 nM, Kd: 40 nM), administered orally. It also serves as an activator of TRPC5 (EC 50: 30 μM) and an inhibitor of TRPM3. This compound, widely used in research, has shown promise in investigating obesity, diabetes, senescence, and ovarian cancer [1] [2] [4] [7]. 在相同实验条件下,摩尔浓度相同的化合物盐形式与游离态具有相同的生物活性,但盐形式 Rosiglitazone hydrochloride 的水溶性和稳定性通常比游离态更好。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 560 | 35日内发货 | ||
10 mg | ¥ 1,060 | 35日内发货 | ||
50 mg | ¥ 4,250 | 35日内发货 | ||
100 mg | ¥ 7,450 | 35日内发货 |
Rosiglitazone potassium 的其他形式现货产品:
产品描述 | Rosiglitazone (BRL 49653) potassium is a potent and selective PPARγ agonist (EC 50: 60 nM, Kd: 40 nM), administered orally. It also serves as an activator of TRPC5 (EC 50: 30 μM) and an inhibitor of TRPM3. This compound, widely used in research, has shown promise in investigating obesity, diabetes, senescence, and ovarian cancer [1] [2] [4] [7]. |
体外活性 | Rosiglitazone potassium (0.1-10 μM, 72 h) results in pluripotent C3H10T1/2 stem cell differentiation to adipocytes [1]. Rosiglitazone potassium (1 μM, 24 h) activates PPARγ, which binds to NF-α1 promoter to activate gene transcription in neurons [3]. Rosiglitazone potassium (1 μM, 24 h) protects Neuro2A cells and hippocampal neurons against oxidative stress, and up-regulates BCL-2 expression in an NF-α1-dependent manner [3]. Rosiglitazone potassium (0.01-100 μM, 15 min) inhibits TRPM3 with IC 50 values of 9.5 and 4.6 μM against nifedipine- and PregS-evoked activity respectively [4]. Rosiglitazone potassium (0.5-50 μM, 7 days) inhibits ovarian cancer cell proliferation [7]. Rosiglitazone potassium (5 μM, 7 days) suppresses Olaparib induced alterations of cellular senescence and promotes apoptosis in A2780 and SKOV3 cells [7]. Cell Proliferation Assay [7] Cell Line: A2780 and SKOV3 cells Concentration: 0.5-50 μM Incubation Time: 1-7 days Result: Inhibited cell proliferation in a time dependent and concentration dependent manner. Western Blot Analysis [3] Cell Line: Hippocampal neurons Concentration: 1 μM Incubation Time: 24 h Result: Increased NF-α1 and BCL-2 protein level. |
体内活性 | Rosiglitazone potassium (oral administration, 5 mg/kg, daily for 8 weeks) decreases the serum glucose in diabetic rats [5]. Rosiglitazone potassium (intraperitoneal injection, 3 mg/kg/day) ameliorates airway inflammation induced by cigarette smoke via inhibiting the M1 macrophage polarization by activating PPARγ and RXRα in male Wistar rats [6]. Rosiglitazone potassium (intraperitoneal injection, 10 mg/kg, once every 2 days) inhibits subcutaneous ovarian cancer growth in A2780 and SKOV3 mouse subcutaneous xenograft models [7]. Animal Model: Streptozotocin (STZ)-induced diabetic rats [5] Dosage: 5 mg/kg Administration: Oral administration, daily for 8 weeks. Result: Decreased IL-6, TNF-α, and VCAM-1 levels in diabetic group. Displayed lower levels of lipid peroxidation and NOx with an increase in aortic GSH and SOD levels compared to diabetic groups. Animal Model: Male Wistar rats [6] Dosage: 3 mg/kg/day Administration: Intraperitoneal injection, twice a day, 6 days per week for 12 consecutive weeks Result: Ameliorated emphysema, elevated PEF, and higher level of total cells, neutrophils and cytokines (TNF-α and IL-1β) induced by cigarette smoke (CS). Inhibited CS-induced M1 macrophage polarization and decreased the ratio of M1/M2. |
分子量 | 395.52 |
分子式 | C18H18KN3O3S |
CAS No. | 316371-84-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Rosiglitazone potassium 316371-84-3 Others Inhibitor inhibitor inhibit