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Gliquidone
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Gliquidone图片
CAS NO:33342-05-1
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
50mg电议

产品介绍
Gliquidone (AR-DF 26) 是磺脲类中的一种抗糖尿病药物，用于治疗 2 型糖尿病。
Cas No.33342-05-1
别名格列喹酮; AR-DF 26
化学名1-cyclohexyl-3-[4-[2-(7-methoxy-4,4-dimethyl-1,3-dioxoisoquinolin-2-yl)ethyl]phenyl]sulfonylurea
Canonical SMILESCC1(C2=C(C=C(C=C2)OC)C(=O)N(C1=O)CCC3=CC=C(C=C3)S(=O)(=O)NC(=O)NC4CCCCC4)C
分子式C27H33N3O6S
分子量527.63
溶解度≥ 22.4mg/mL in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Gliquidone is an antagonist of ATP-sensitive K+ channel with IC50 value of 27.2 nM [1].

ATP-sensitive K+ channel is a type of K+ channel that is gated by intracellular ATP and ADP. ATP-sensitive K+ channel mainly exists in plasma membrane.

Gliquidone is an ATP-sensitive K+ channel antagonist. In mice, gliquidone (10 or 40 μg) antagonized morphine (20 mg/kg) induced hypermotility in a dose-dependent way. These results suggested that ATP-sensitive K+ channels played an important role in morphine-induced hypermotility [1]. In mice, gliquidone (2-8 μg) antagonized the antinociceptive effect induced by R-PIA (the adenosine A1 receptor agonist) in a dose-dependent way, which suggested that ATP-sensitive K+ channels mediated antinociception induced by R-PIA [2].

In patients with type 2 diabetes mellitus, gliquidone reduced the mean plasma glucose levels by 15% and increased insulin levels by 40% [3]. In Caucasian patients with new-onset diabetes mellitus (NODM) after kidney transplantation, gliquidone reduced fasting blood glucose (FBG) from 154 mg/dl to 120 mg/dl [4].

References:
[1].  Ocana M, Del Pozo E, Baeyens JM. Gliquidone, an ATP-dependent K+ channel antagonist, antagonizes morphine-induced hypermotility. Eur J Pharmacol, 1993, 239(1-3): 253-255.
[2].  Ocana M, Baeyens JM. Role of ATP-sensitive K+ channels in antinociception induced by R-PIA, an adenosine A1 receptor agonist. Naunyn Schmiedebergs Arch Pharmacol, 1994, 350(1): 57-62.
[3].  von Nicolai H, Brickl R, Eschey H, et al. Duration of action and pharmacokinetics of the oral antidiabetic drug gliquidone in patients with non-insulin-dependent (type 2) diabetes mellitus. Arzneimittelforschung, 1997, 47(3): 247-252.
[4].  Tuerk TR, Bandur S, Nuernberger J, et al. Gliquidone therapy of new-onset diabetes mellitus after kidney transplantation. Clin Nephrol, 2008, 70(1): 26-32.