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首页 / 抑制剂/激动剂 / 膜转运蛋白 / 钾通道 / Mitiglinide calcium

米格列奈钙 /Mitiglinide calcium {[allProObj[0].p_purity_real_show]}

货号：A127678 同义名： 米格列奈 / S21403 anhydrous;KAD-1229 anhydrous Ambeed 开学季，买赠积分，赢豪礼

Mitiglinide calcium is a blood glucose-lowering drugs, stimulating insulin secretion by closing the ATP-sensitive K+ channels in pancreatic beta-cells.

Mitiglinide calcium 化学结构 CAS号：145525-41-3
Mitiglinide calcium 化学结构
CAS号：145525-41-3
Mitiglinide calcium 3D分子结构
CAS号：145525-41-3
Mitiglinide calcium 化学结构 CAS号：145525-41-3
Mitiglinide calcium 3D分子结构 CAS号：145525-41-3
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Mitiglinide calcium 纯度/质量文件 产品仅供科研

货号：A127678 标准纯度： {[allProObj[0].p_purity_real_show]}
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产品名称 Potassium Channel ↓ 其他靶点 纯度
Tolbutamide ✔ {[allProObj[0].p_purity_real_show]}
Glimepiride ++++

SUR2B, IC50: 7.3 nM

SUR1, IC50: 5.4 nM

 		{[allProObj[0].p_purity_real_show]}
Dronedarone Hydrochloride ✔ {[allProObj[0].p_purity_real_show]}
Gliquidone ++

Potassium channel, IC50: 27.2 nM

 		{[allProObj[0].p_purity_real_show]}
TRAM-34 +++

IKCa1 (KCa3.1), Kd: 20 nM

 		{[allProObj[0].p_purity_real_show]}
Glibenclamide ✔ {[allProObj[0].p_purity_real_show]}
Amiodarone HCl ✔ {[allProObj[0].p_purity_real_show]}
Gliclazide ++

Potassium channel, IC50: 184 nM

 		{[allProObj[0].p_purity_real_show]}
Repaglinide ✔ {[allProObj[0].p_purity_real_show]}
Dofetilide ✔ {[allProObj[0].p_purity_real_show]}
Nateglinide ✔ {[allProObj[0].p_purity_real_show]}
Quinine hydrochloride dihydrate ✔ {[allProObj[0].p_purity_real_show]}
ML133 HCl +

Kir2.1, IC50: 290 nM

 		{[allProObj[0].p_purity_real_show]}
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。

Mitiglinide calcium 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].

Mitiglinide calcium 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 <<

Mitiglinide calcium 参考文献

[1]Arao T, Okada Y, et al. Comparison Between Effectiveness of 100 mg/day Sitagliptin and a Switch to Mitiglinide Calcium Hydrate/Voglibose from 50 mg/day Sitagliptin in Patients with Type 2 Diabetes. J UOEH. 2017;39(1):1-9.

[2]Mogami H, Shibata H, et al. Inhibition of ATP-sensitive K+ channel by a non-sulfonylurea compound KAD-1229 in a pancreatic beta-cell line, MIN 6 cell. Eur J Pharmacol. 1994 Nov 15;269(3):293-8.

[3]Ojima K, Kiyono Y, Kojima M. Nihon Yakurigaku Zasshi. 2004;124(4):245-255

[4]Li H, Kim HW, Shin SE, et al. The vasorelaxant effect of mitiglinide via activation of voltage-dependent K+ channels and SERCA pump in aortic smooth muscle. Life Sci. 2017;188:1-9

Mitiglinide calcium 实验方案

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

Mitiglinide calcium 技术信息

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

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
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

Tags: Mitiglinide | 145525-41-3 | KAD-1229 | S21403 | KAD1229 | KAD 1229 | S 21403 | S-21403 | K(ATP) Channel Antagonist | Membrane Transporter/Ion Channel | Potassium Channel | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Mitiglinide calcium 纯度/质量文件 | Mitiglinide calcium 亚型比较 | Mitiglinide calcium 生物活性 | Mitiglinide calcium 临床数据 | Mitiglinide calcium 参考文献 | Mitiglinide calcium 实验方案 | Mitiglinide calcium 技术信息

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