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Merck
CN

G0326000

格列齐特

European Pharmacopoeia (EP) Reference Standard

别名:

1-(3-氮杂双环[3.3.0]辛-3-基)-3-对甲苯磺酰脲

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About This Item

经验公式(希尔记法):
C15H21N3O3S
CAS号:
分子量:
323.41
MDL编号:
UNSPSC代码:
41116107
PubChem化学物质编号:
NACRES:
NA.24

等级

pharmaceutical primary standard

API类

gliclazide

制造商/商品名称

EDQM

mp

163-169 °C (lit.)

应用

pharmaceutical (small molecule)

包装形式

neat

储存温度

2-8°C

SMILES字符串

Cc1ccc(cc1)S(=O)(=O)NC(=O)NN2CC3CCCC3C2

InChI

1S/C15H21N3O3S/c1-11-5-7-14(8-6-11)22(20,21)17-15(19)16-18-9-12-3-2-4-13(12)10-18/h5-8,12-13H,2-4,9-10H2,1H3,(H2,16,17,19)

InChI key

BOVGTQGAOIONJV-UHFFFAOYSA-N

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一般描述

This product is provided as delivered and specified by the issuing Pharmacopoeia. All information provided in support of this product, including SDS and any product information leaflets have been developed and issued under the Authority of the issuing Pharmacopoeia.For further information and support please go to the website of the issuing Pharmacopoeia.

应用

用于治疗非胰岛素依赖型糖尿病(NIDDM)。

生化/生理作用

低密度脂蛋白(LDL)的氧化修饰在与糖尿病相关的血管功能障碍中起重要作用。格列齐特是具有清除自由基活性的第二代磺酰脲类药物。在增加浓度的格列齐特(1 至 10 μg/mL)存在下,将人主动脉平滑肌细胞(HASMC)与天然人 LDL(100 μg/mL)一起孵育会导致 HASMC 介导的 LDL 氧化剂量依赖性降低。HASMC暴露于格列齐特(1 至 10 μg/mL)和天然 LDL(100 μg/mL)中也导致氧化的 LDL 诱导的人类单核细胞与 HASMC粘附的剂量依赖性降低。此外,将 HASMC 与格列齐特一起孵育会大大降低氧化的 LDL 次级这些细胞增殖的能力。最后,在基因和蛋白质水平上,使用格列齐特处理 HASMC,将导致氧化修饰的 LDL 诱导的单核细胞趋化蛋白(MCP)-1 和人热休克蛋白 70(HSP 70)的表达显着降低。这些结果表明,格列齐特,浓度在治疗范围内(5 至 10 μg/mL)时,在体外可有效减轻氧化修饰的 LDL 引起的血管平滑肌细胞(VSMC)功能障碍。对 2 型糖尿病患者给予格列齐特可能成为预防和管理糖尿病心血管疾病策略的一部分

包装

The product is delivered as supplied by the issuing Pharmacopoeia. For the current unit quantity, please visit the EDQM reference substance catalogue.

其他说明

Sales restrictions may apply.

象形图

Exclamation mark

警示用语:

Warning

危险声明

危险分类

Acute Tox. 4 Oral

储存分类代码

11 - Combustible Solids

WGK

WGK 2

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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K G Alberti
Diabete & metabolisme, 20(3 Pt 2), 341-348 (1994-11-01)
Gliclazide is a second-generation sulfonylures that is widely used in the treatment of non-insulin-dependent diabetes mellitus (Type 2 diabetes). It has been recommended for use on the basis of both its metabolic and nonmetabolic effects. It has a clear beneficial
P E Jennings
Journal of diabetes and its complications, 8(4), 226-230 (1994-10-01)
Patients with type II diabetes commonly die from thrombotic vascular disease. Large vessel occlusion due to thrombosis or atherosclerotic stenosis is a process accelerated by diabetes and results in premature death. Diabetic small vessel disease, with its unique microangiopathic process
A Avogaro
Diabetes, obesity & metabolism, 14 Suppl 1, 14-19 (2011-12-14)
Type 2 diabetes mellitus (T2DM) is a progressive disease characterized by worsening hyperglycaemia. Lowering haemoglobin A1c to below or around 7% has been shown to reduce microvascular and neuropathic complications of diabetes. The ongoing uncertainty regarding whether intensive glycaemic control
P E Jennings
Metabolism: clinical and experimental, 49(10 Suppl 2), 17-20 (2000-11-15)
Advanced glycolysation end products (AGEs) and the free radicals generated in this process can both be implicated in the accelerated atherosclerosis and vascular and prothrombotic microangiopathic changes typified by diabetes. The rate of formation of free radicals is dependent on
Guntram Schernthaner
Metabolism: clinical and experimental, 52(8 Suppl 1), 29-34 (2003-08-27)
Gliclazide modified release (MR) is a new formulation of the drug gliclazide and is given once daily. The specifically designed hydrophilic matrix of gliclazide MR leads to a progressive drug release that parallels the 24-hour glycemic profile in type 2

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