G2295
格列美脲
≥98% (HPLC), insulin secretagogue, solid
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关于此项目
经验公式（希尔记法）:
C24H34N4O5S
化学文摘社编号:
分子量:
490.62
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
产品名称
格列美脲, ≥98% (HPLC), solid
质量水平
方案
≥98% (HPLC)
表单
solid
颜色
white
mp
212.2-214.5 °C
溶解性
DMSO: >10 mg/mL
创始人
Sanofi Aventis
储存温度
room temp
SMILES字符串
CCC1=C(C)CN(C(=O)NCCc2ccc(cc2)S(=O)(=O)NC(=O)N[C@H]3CC[C@H](C)CC3)C1=O
InChI
1S/C24H34N4O5S/c1-4-21-17(3)15-28(22(21)29)24(31)25-14-13-18-7-11-20(12-8-18)34(32,33)27-23(30)26-19-9-5-16(2)6-10-19/h7-8,11-12,16,19H,4-6,9-10,13-15H2,1-3H3,(H,25,31)(H2,26,27,30)/t16-,19-
InChI key
WIGIZIANZCJQQY-RUCARUNLSA-N
基因信息
human ... ABCC8(6833), KCNJ1(3758), KCNJ11(3767)
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相关类别
一般描述
格列美脲属于生物制药II类二代磺酰脲类药物。
应用
格列美脲已被用于：
- 作为一种降糖药物用于测试其在人脐静脉细胞（HUVEC）中的抗糖尿病功能
- 在乳腺癌MDA-MB-231细胞中作为磺酰脲类ATP敏感型钾通道（KATP）抑制剂
- 在新生儿胰岛样细胞簇（NICC）的葡萄糖刺激胰岛素分泌（GSIS）测定中检测其对胰岛素分泌的影响
格列美脲目前用于治疗 2 型糖尿病。
生化/生理作用
心脏 KATP 通道的强力阻断剂。
格列美脲可通过刺激胰腺β细胞分泌胰岛素激素来降低血糖水平。它可与与β细胞相关的一种65-kD蛋白发生相互作用。
格列美脲是一种有效的心肌梗死 KATP 通道阻断剂，被吡那地尔激活，IC50 值为 6.8 nM。
特点和优势
该化合物由Sanofi Aventis开发。要浏览其他药物开发化合物和批准的药物/候选药物列表，单击此处。
警示用语：
Warning
危险声明
危险分类
Repr. 2
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
Eyeshields, Gloves, type N95 (US)
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Li-Ping Wang et al.
Cellular physiology and biochemistry : international journal of experimental cellular physiology, biochemistry, and pharmacology, 38(6), 2337-2347 (2016-05-21)
By inducing severe endothelial impairment, hypertension and diabetes are two leading causes of morbidity and mortality. Hypertensive patients with concomitant diabetes must take both antihypertensive and hypoglycaemic medications, for which there is a lack of experimental and clinical guidelines. This
A REVIEW ARTICLE ON GLIMEPERIDE: AN ORAL HYPOGLYCAEMIC DRUG
Tiwari A, et al.
International Journal of Advanced Research , 4, 920-927 (2016)
William T Cefalu et al.
Lancet (London, England), 382(9896), 941-950 (2013-07-16)
Sodium-glucose cotransporter 2 (SGLT2) inhibitors improve glycaemia in patients with type 2 diabetes by enhancing urinary glucose excretion. We compared the efficacy and safety of canagliflozin, an SGLT2 inhibitor, with glimepiride in patients with type 2 diabetes inadequately controlled with
W Rathmann et al.
Diabetes, obesity & metabolism, 15(1), 55-61 (2012-08-07)
To investigate therapy persistence, frequency of hypoglycaemia and macrovascular outcomes among type 2 diabetes patients with dipeptidyl peptidase-4 (DPP-4) inhibitors (DPP-4) and sulphonylureas (SU). Data from 19,184 DPP-4 (mean age: 64 years; 56% males) and 31,110 SU users (69 years;
Mitsuyoshi Takahara et al.
Endocrine journal, 59(12), 1131-1136 (2012-08-02)
We retrospectively investigated the effect of adding dipeptidyl peptidase-4 (DPP-4) inhibitor and tapering sulfonylurea on blood glucose fluctuation in Asian patients with type 2 diabetes mellitus under basal-supported oral therapy (BOT). We recruited twenty-two consecutive Japanese patients with type 2
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