产品说明书
Mitiglinide calcium
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同义名 : | 米格列奈 ;S21403 anhydrous;KAD-1229 anhydrous;S21403;KAD-1229;Mitiglinide (calcium salt) |
| CAS号 : | 145525-41-3 | |
| 货号 : | A127678 | |
| 分子式 : | C38H48CaN2O6 | |
| 纯度 : | 98% | |
| 分子量 : | 668.875 | |
| MDL号 : | MFCD09263183 | |
| 存储条件： |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 4 mg/mL(5.98 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 |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Mitiglinide Calcium is a drug for the treatment of type 2 diabetes; it is a highly selective KATP channel antagonist. Mitiglinide is thought to stimulate insulin secretion by closing the ATP-sensitive K(+) (KATP) channels in pancreatic beta-cells, and its early insulin release and short duration of action would be effective in improving postprandial hyperglycemia. Mitiglinide shows a higher selectivity for the beta-cell type of SUR1/Kir6.2 than the cardiac and smooth muscle types of K(ATP) channels in comparison with glibenclamide and glimepiride. Insulinotropic effect of mitiglinide is more potent than that of nateglinide, and mitiglinide surpassed in controlling postprandial hyperglycemia in normal and diabetic animals. In clinical trials, treatment with mitiglinide provided lasting improvement of postprandial hyperglycemia in Type 2 diabetic patients and decreased the fasting plasma glucose levels and HbA(1C) values[3]. Mitiglinide induces vasorelaxation via activation of Kv channels and SERCA (sarcoplasmic/endoplasmic reticulum Ca2+-ATPase) pump. However, the vasorelaxant effects of mitiglinide did not involve other K+ channels, Ca2+ channels, PKA/PKG signaling pathways, or the endothelium[4]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT01456130 | Diabetes Mellitus | Phase 3 | Completed | - | Japan ... 展开 >> Nagoya-shi, Aichi, Japan Fukuoka-shi, Fukuoka, Japan Kurume-shi, Fukuoka, Japan Sapporo-shi, Hokkaido, Japan Kobe-shi, Hyogo, Japan Kagoshima-shi, Kagoshima, Japan Kumamoto-shi, Kumamoto, Japan Osaki-shi, Miyagi, Japan Minou-shi, Osaka, Japan Osaka-shi, Osaka, Japan Kamio-shi, Saitama, Japan Koshigaya-shi, Saitama, Japan Adachi-ku, Tokyo, Japan Chuo-ku, Tokyo, Japan 收起 << |
| NCT01456130 | - | Completed | - | - | |
| NCT01403818 | Healthy Pharm... 展开 >>acokinetics of ASP1941 Pharmacokinetics of Mitiglinide 收起 << | Phase 1 | Completed | - | Japan ... 展开 >> Kantou, Japan 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.50mL 0.30mL 0.15mL |
7.48mL 1.50mL 0.75mL |
14.95mL 2.99mL 1.50mL |
| 参考文献 |
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[3]Ojima K, Kiyono Y, Kojima M. Nihon Yakurigaku Zasshi. 2004;124(4):245-255 |