货号:A127678 同义名: 米格列奈 / S21403 anhydrous;KAD-1229 anhydrous
Mitiglinide calcium是一种降血糖药物,通过关闭胰岛β细胞中的ATP敏感的K+通道刺激胰岛素分泌。
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产品名称 | Potassium Channel ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Tolbutamide | ✔ | 98% | |||||||||||||||||
Glimepiride |
++++
SUR1, IC50: 5.4 nM SUR2B, IC50: 7.3 nM |
97% | |||||||||||||||||
Dronedarone Hydrochloride | ✔ | 95% | |||||||||||||||||
Gliquidone |
++
Potassium channel, IC50: 27.2 nM |
99% | |||||||||||||||||
TRAM-34 |
+++
IKCa1 (KCa3.1), Kd: 20 nM |
98% | |||||||||||||||||
Glibenclamide | ✔ | 98% | |||||||||||||||||
Amiodarone HCl | ✔ | 97% | |||||||||||||||||
Gliclazide |
++
Potassium channel, IC50: 184 nM |
98% | |||||||||||||||||
Repaglinide | ✔ | 98% | |||||||||||||||||
Dofetilide | ✔ | 98% | |||||||||||||||||
Nateglinide | ✔ | 99% | |||||||||||||||||
Quinine hydrochloride dihydrate | ✔ | 98% | |||||||||||||||||
ML133 HCl |
+
Kir2.1, IC50: 290 nM |
99% | |||||||||||||||||
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 | 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]. |
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 << |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.50mL 0.30mL 0.15mL |
7.48mL 1.50mL 0.75mL |
14.95mL 2.99mL 1.50mL |
CAS号 | 145525-41-3 |
分子式 | C38H48CaN2O6 |
分子量 | 668.875 |
别名 | 米格列奈 ;S21403 anhydrous;KAD-1229 anhydrous;S21403;KAD-1229;Mitiglinide (calcium salt) |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Inert atmosphere,Room Temperature |
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 |
动物实验配方 |