产品说明书

Gliquidone

Print
Chemical Structure| 33342-05-1 同义名 : AR-DF 26
CAS号 : 33342-05-1
货号 : A559869
分子式 : C27H33N3O6S
纯度 : 98%
分子量 : 527.632
MDL号 : MFCD00631870
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(94.76 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：

2% DMSO+corn oil 5 mg/mL

生物活性
靶点

  • Potassium Channel

    Potassium channel, IC50:27.2 nM
描述 Gliquidone, a sulfonylurea class drug used for treating diabetes mellitus type 2. Gliquidone reduced the body weight and the kidney weight/body weight ratio of mice. Gliquidone improved the kidney function, indicated by reductions in urinary protein, blood urea nitrogen, and serum creatinine and triglyceride. Gliquidone can ameliorate the diabetic symptoms of diabetic nephropathy through inhibiting Notch/Snail1 signaling pathway, improving anti-oxidative response and delaying renal interstitial fibrosis[3]. Gliquidone treatment effectively reduced urinary protein in GK rats with diabetic nephropathy by improving glomerular lesions and promoting tubular reabsorption[4]. Moreover, using gliquidone nanoparticles revealed ~2.5-fold increase in Cmax when taken orally in the form of hard gelatin capsules in comparison to free gliquidone. The developed strategy of gliquidone nanoparticles possess a keen potential for exhibiting anti-diabetic effect[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
NCT02476760 - 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 <<
NCT00568074 Diabetes Diab... 展开 >>etes Mellitus, Type 2 收起 << Phase 4 Completed - China, Shanghai ... 展开 >> Novo Nordisk Investigational Site Shanghai, Shanghai, China, 200025 Novo Nordisk Investigational Site Shanghai, Shanghai, China, 200433 China, Sichuan Novo Nordisk Investigational Site Chengdu, Sichuan, China, 610041 China Novo Nordisk Investigational Site Beijing, China, 100029 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.90mL

0.38mL

0.19mL

9.48mL

1.90mL

0.95mL

18.95mL

3.79mL

1.90mL
参考文献

[1]Galeotti N, Ghelardini C, et al. Involvement of potassium channels in amitriptyline and clomipramine analgesia. Neuropharmacology. 2001;40(1):75-84.

[2]Ocana M, Del Pozo E, et al. Subgroups among mu-opioid receptor agonists distinguished by ATP-sensitive K+ channel-acting drugs. Br J Pharmacol. 1995 Mar;114(6):1296-302.

[3]Tian H, Yang J, Xie Z, Liu J. Gliquidone Alleviates Diabetic Nephropathy by Inhibiting Notch/Snail Signaling Pathway. Cell Physiol Biochem. 2018;51(5):2085-2097

[4]Ke JT, Li M, Xu SQ, et al. Gliquidone decreases urinary protein by promoting tubular reabsorption in diabetic Goto-Kakizaki rats. J Endocrinol. 2014;220(2):129-141. Published 2014 Jan 8

[5]Mohamed MS, Abdelhafez WA, Zayed G, Samy AM. Optimization, in-vitro Release and in-vivo Evaluation of Gliquidone Nanoparticles. AAPS PharmSciTech. 2019;21(2):35. Published 2019 Dec 26