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Glimepiride

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Chemical Structure| 93479-97-1 同义名 : Glimperide;HOE-490;Roname;Lacer brand of glimepiride;Hoechst brand of glimepiride;Glimepiridum;Glimepirida;Amarel;Amaryl
CAS号 : 93479-97-1
货号 : A552202
分子式 : C24H34N4O5S
纯度 : 97%
分子量 : 490.616
MDL号 : MFCD00878417
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(71.34 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：
生物活性
靶点

  • Potassium Channel

    SUR1, IC50:5.4 nM

    SUR2B, IC50:7.3 nM
描述 Glimepiride (Hoe 490) is a new sulfonylurea. After oral administration of Hoe 490 to rabbits, blood glucose was lowered 3.5 times more than after glibenclamide (HB 419) and after intravenous administration, 2.5 times more. The more rapid decrease in blood glucose in the dog after oral administration of glimepiride was accompanied by a correspondingly earlier and higher plasma insulin increase[3]. Glimepiride is a second-generation sulfonylurea that stimulates pancreatic β cells to release insulin. It can also be combined with other antihyperglycemic agents, including metformin and insulin, in patients who are not adequately controlled by sulfonylureas alone[4]. Glimepiride decreased extracellular Aβ40 and Aβ42 levels. The effect of glimepiride on reduction of Aβ40 generation was mediated by downregulation of β-site APP-cleaving enzyme 1 (BACE1) mRNA and protein expression, and by suppression of BACE1 activity[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.04mL

0.41mL

0.20mL

10.19mL

2.04mL

1.02mL

20.38mL

4.08mL

2.04mL
参考文献

[1]Lawrence CL, Rainbow RD, et al. Effect of metabolic inhibition on glimepiride block of native and cloned cardiac sarcolemmal K(ATP) channels. Br J Pharmacol. 2002 Jul;136(5):746-52.

[2]Song DK, Ashcroft FM. Glimepiride block of cloned beta-cell, cardiac and smooth muscle K(ATP) channels. Br J Pharmacol. 2001 May;133(1):193-9.

[3]Geisen K. Special pharmacology of the new sulfonylurea glimepiride. Arzneimittelforschung. 1988;38(8):1120-1130

[4]Basit A, Riaz M, Fawwad A. Glimepiride: evidence-based facts, trends, and observations (GIFTS). [corrected] [published correction appears in Vasc Health Risk Manag. 2013;9:1]. Vasc Health Risk Manag. 2012;8:463-472

[5]Liu F, Wang Y, Yan M, Zhang L, Pang T, Liao H. Glimepiride attenuates Aβ production via suppressing BACE1 activity in cortical neurons. Neurosci Lett. 2013;557 Pt B:90-94