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

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。

Mitiglinide calcium/米格列奈钙 化学结构 CAS号:145525-41-3
Mitiglinide calcium/米格列奈钙 化学结构
CAS号:145525-41-3
Mitiglinide calcium/米格列奈钙 3D分子结构
CAS号:145525-41-3
Mitiglinide calcium/米格列奈钙 化学结构 CAS号:145525-41-3
Mitiglinide calcium/米格列奈钙 3D分子结构 CAS号:145525-41-3
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Mitiglinide calcium/米格列奈钙 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 98%
Glimepiride ++++

SUR2B, IC50: 7.3 nM

SUR1, IC50: 5.4 nM

97%
Dronedarone HCl 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 HCl 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。

Mitiglinide calcium/米格列奈钙 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/米格列奈钙 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/米格列奈钙 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/米格列奈钙 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/米格列奈钙 技术信息

CAS号145525-41-3
分子式C38H48CaN2O6
分子量 668.88
SMILES Code O=C([O-])[C@@H](CC1=CC=CC=C1)CC(N2C[C@@]3([H])CCCC[C@@]3([H])C2)=O.O=C([O-])[C@@H](CC4=CC=CC=C4)CC(N5C[C@@]6([H])CCCC[C@@]6([H])C5)=O.[Ca+2]
MDL No. MFCD09263183
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 Sealed in dry,2-8°C

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
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