Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Mizagliflozin (GSK-1614235 free base) 是口服有效的、选择性的 SGLT1抑制剂,对人 SGLT1 的 Ki 值为 27 nM。Mizagliflozin 对 SGLT1 的选择性是 SGLT2的303 倍。它是抗糖尿病药物,可以改善餐后血糖波动。它在改善慢性便秘方面具有潜在的作用。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 678 | 现货 | ||
2 mg | ¥ 995 | 现货 | ||
5 mg | ¥ 1,620 | 现货 | ||
10 mg | ¥ 2,860 | 现货 | ||
25 mg | ¥ 4,760 | 现货 | ||
50 mg | ¥ 6,780 | 现货 | ||
100 mg | ¥ 9,180 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,980 | 现货 |
产品描述 | Mizagliflozin (GSK-1614235 free base) is a sodium-glucose transporter inhibitor( Ki of 27 nM for human SGLT1). Mizagliflozin displays 303-fold selectivity over SGLT2. Mizagliflozin is used as an antidiabetic drug that can modify postprandial blood glucose excursion. Mizagliflozin also exhibits potential in the amelioration of chronic constipation. |
靶点活性 | SGLT1 (human):(ki)27 nM, SGLT2 (human):8170 nM(ki) |
体内活性 | Mizagliflozin, a novel selective sodium glucose co-transporter 1 (SGLT1) inhibitor, for the amelioration of chronic constipation.?Mizagliflozin's inhibitory activity against SGLTs was evaluated by an in vitro assay of cells transiently expressing SGLTs.?The safety profile of an initial single dose (2-160mg, orally) and multiple doses (2-20mg, orally, once daily immediately prior to breakfast on Days 1 and 13, and three times daily immediately prior to every meal on Days 3-12) of mizagliflozin was determined by performing a phase I study in healthy male subjects.?In addition, the effect of mizagliflozin and lubiprostone on fecal wet weight was compared using a dog model of loperamide-induced constipation and rat model of low-fiber-diet-induced constipation.?Mizagliflozin potently inhibited human SGLT1 in a highly selective manner.?The results of the phase I study showed mizagliflozin increased stool frequency and loosened stool consistency;?these effects increased progressively with an increase in the dosage and the number of doses of mizagliflozin.?In addition, the oral administration of mizagliflozin increased fecal wet weight in a dog model of loperamide-induced constipation and a rat model of low-fiber-diet-induced constipation, similar to lubiprostone.?The potential use of a novel selective SGLT1 inhibitor, mizagliflozin, for the amelioration of chronic constipation[1]. |
别名 | GSK-1614235 free base, KGA-3235 free base, DSP-3235 free base |
分子量 | 564.67 |
分子式 | C28H44N4O8 |
CAS No. | 666843-10-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Methanol: 250 mg/mL (442.74 mM), Sonication is recommended.
DMSO: 100 mg/mL (177.09 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Methanol / DMSO | 1 mM | 1.7709 mL | 8.8547 mL | 17.7095 mL | 44.2736 mL |
5 mM | 0.3542 mL | 1.7709 mL | 3.5419 mL | 8.8547 mL | |
10 mM | 0.1771 mL | 0.8855 mL | 1.7709 mL | 4.4274 mL | |
20 mM | 0.0885 mL | 0.4427 mL | 0.8855 mL | 2.2137 mL | |
50 mM | 0.0354 mL | 0.1771 mL | 0.3542 mL | 0.8855 mL | |
100 mM | 0.0177 mL | 0.0885 mL | 0.1771 mL | 0.4427 mL |
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。
Mizagliflozin 666843-10-3 GPCR/G Protein SGLT Chronic GSK1614235 DSP3235 DSP-3235 KGA3235 selective Sodium-dependent glucose cotransporters constipation GSK-1614235 free base DSP 3235 antidiabetic disorder KGA-3235 free base gastrointestinal DSP-3235 free base GSK 1614235 inhibit GSK-1614235 KGA-3235 Inhibitor KGA 3235 inhibitor