货号:A1167800 同义名: DSP-3235 free base;KGA-3235 free base
Mizagliflozin是一种高效的 SGLT1 抑制剂,通过抑制小肠中的钠-葡萄糖共转运蛋白,改善餐后血糖水平,并有助于慢性便秘的治疗。它在糖尿病和胃肠道疾病的研究中具有应用前景。
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产品名称 | SGLT1 ↓ ↑ | SGLT2 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Phloretin | ✔ | 98% | |||||||||||||||||
Canagliflozin |
+++
hSGLT2, IC50: 3.7 nM mSGLT2, IC50: 2 nM |
95% | |||||||||||||||||
Empagliflozin |
++
SGLT2, IC50: 3.1 nM |
98% | |||||||||||||||||
Dapagliflozin |
++++
hSGLT2, EC50: 1.1 nM |
97% | |||||||||||||||||
Tofogliflozin (hydrate) |
+++
hSGLT2, IC50: 2.9 nM |
99%+ | |||||||||||||||||
Sotagliflozin |
+
SGLT1, IC50: 36 nM |
++++
SGLT2, IC50: 1.8 nM |
98% | ||||||||||||||||
Ipragliflozin |
++
hSGLT2, IC50: 7.4 nM |
98% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Mizagliflozin (DSP-3235 free base) is a potent, orally active inhibitor specifically targeting the SGLT1 transporter, with a Ki of 27 nM for human SGLT1, showcasing a 303-fold selectivity over SGLT2. This selectivity positions Mizagliflozin as a promising antidiabetic agent capable of modifying postprandial blood glucose levels. Additionally, it has shown potential in alleviating symptoms of chronic constipation[1]. |
体内研究 | Administered orally in dosages ranging from 3 to 30 mg/kg, Mizagliflozin demonstrates a laxative effect[1]. When administered either intravenously at 0.3 mg/kg or orally at 3 mg/kg, Mizagliflozin is characterized by a short half-life, 0.23 hours and 1.14 hours respectively, indicating its rapid elimination from the body[2]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.77mL 0.35mL 0.18mL |
8.85mL 1.77mL 0.89mL |
17.71mL 3.54mL 1.77mL |
CAS号 | 666843-10-3 |
分子式 | C28H44N4O8 |
分子量 | 564.671 |
别名 | DSP-3235 free base;KGA-3235 free base;GSK-1614235;KGA-3235;DSP 3235;DSP-3235, DSP3235;KWA 0711;GSK-1614235 free base |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,2-8°C |
溶解度 |
DMSO: 105 mg/mL(185.95 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO H2O: 100 mg/mL(177.09 mM) |
动物实验配方 |