Glipizide

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Chemical Structure| 29094-61-9 同义名 : 格列甲嗪 ;K 4024;CP 28720;Ozidia;Minodiab;Melizide;Glydiazinamide;Minidiab;Glucotrol;TK 1320
CAS号 : 29094-61-9
货号 : A625260
分子式 : C21H27N5O4S
纯度 : 99%
分子量 : 445.535
MDL号 : MFCD00072159
存储条件：

Pure form Sealed in dry,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(112.22 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
描述 Glipizide is used to treat high blood sugar levels caused by a type of diabetes mellitus called type 2 diabetes. It is classified as a second generation sulfonylurea, which means that it undergoes enterohepatic circulation. Mechanism of action is produced by blocking potassium channels in the beta cells of the islets of Langerhans. By partially blocking the potassium channels, the cell remains depolarized, increasing the time the cell spends in the calcium release stage, which results in signaling leading to calcium influx. The increase in calcium will initiate more insulin release from each beta cell. Sulfonylureas may also cause the decrease of serum glucagon and potentiate the action of insulin at the extrapancreatic tissues[3]. Glipizide treatment decreased dilated renal tubule number, improved glomerulus integrity, and reduced inflammatory infiltration. Glipizide blocks renal interstitial fibrosis by inhibiting AKT signaling pathway[4]. Glipizide release from mucoadhesive microcapsules was slow and extended over longer periods of time and depended on composition of the coat. In the in vivo evaluation, alginate-Carbopol microcapsules could sustain the hypoglycemic effect of glipizide over a 14-hour period[5].
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
NCT02456428 - Completed - Canada, Quebec ... 展开 >> Lady Davis Institute for Medical Research, Jewish General Hospital Montreal, Quebec, Canada, H3T1E2 收起 <<
NCT02475499 - Completed - Canada, Quebec ... 展开 >> Lady Davis Institute for Medical Research, Jewish General Hospital Montreal, Quebec, Canada, H3T1E2 收起 <<
NCT03492580 - Completed - United States, New Jersey ... 展开 >> Janssen Investigative Site Titusville, New Jersey, United States, 08560 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.24mL

0.45mL

0.22mL

11.22mL

2.24mL

1.12mL

22.44mL

4.49mL

2.24mL
参考文献

[1]Rao NG, Menezes RG, et al. Suicide by combined insulin and glipizide overdose in a non-insulin dependent diabetes mellitus physician: a case report. Med Sci Law. 2006 Jul;46(3):263-9.

[2]Chowdary KP, Rao YS. Design and in vitro and in vivo evaluation of mucoadhesive microcapsules of glipizide for oral controlled release: a technical note. AAPS PharmSciTech. 2003;4(3):E39.

[3]Rao NG, Menezes RG, Nagesh KR, Kamath GS. Suicide by combined insulin and glipizide overdose in a non-insulin dependent diabetes mellitus physician: a case report. Med Sci Law. 2006;46(3):263-269

[4]Yang G, Zeng G, Wu JP, et al. Glipizide blocks renal interstitial fibrosis by inhibiting AKT signaling pathway. Eur Rev Med Pharmacol Sci. 2017;21(4):867-872

[5]Chowdary KP, Rao YS. Design and in vitro and in vivo evaluation of mucoadhesive microcapsules of glipizide for oral controlled release: a technical note. AAPS PharmSciTech. 2003;4(3):E39