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Tolazamide

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Chemical Structure| 1156-19-0 同义名 : 托拉唑胺 ;U-17835;NSC 70762;Tolazamide, Tolinase, Norglycin, Tolanase, Tolazolamide
CAS号 : 1156-19-0
货号 : A899724
分子式 : C14H21N3O3S
纯度 : 99%+
分子量 : 311.4
MDL号 : MFCD00083504
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 40 mg/mL(128.45 mM)，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 Tolazamide is an intermediate-acting, first-generation sulfonylurea with hypoglycemic activity. Tolazamide had two general classes of binding sites (i.e., high and low affinity) for normal and glycated HSA. The higher affinity sites had binding constants of around 4.3-6.0 × 104 M-1 for these interactions at pH 7.4 and 37 °C, while the lower affinity sites had binding strengths of 4.9-9.1 × 103 M-1[3]. Tolazamide in vitro alters postreceptor insulin action without influencing the receptor, and suggests insulin-stimulated hexose transport as the cellular process responsible for the hypoglycemic effect of sulfonyureas in adipose tissue[4]. Tolazamide markedly enhances ECM (extracellular matrix) synthesis and accumulation in MCs (mesangial cells) probably by stimulating GLUT1 expression, glucose transport and TGF-beta 1 secretion, irrespective of the ambient glucose concentration. This effect was dose-dependent and minimally inducible by metformin[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 <<
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 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.21mL

0.64mL

0.32mL

16.06mL

3.21mL

1.61mL

32.11mL

6.42mL

3.21mL
参考文献

[1]Schmitt JK, Johns SB. Altering therapy of type II diabetes mellitus from insulin to tolazamide increases blood pressure in spite of weight loss. Am J Hypertens. 1995 May;8(5 Pt 1):520-3.

[2]Sanders R, Faro B, et al. Adjunctive use of tolazamide in newly-diagnosed diabetic children. Horm Metab Res. 1990 Nov;22(11):576-80.

[3]Tao P, Li Z, Woolfork AG, Hage DS. Characterization of tolazamide binding with glycated and normal human serum albumin by using high-performance affinity chromatography. J Pharm Biomed Anal. 2019 Mar 20;166:273-280

[4]Maloff BL, Lockwood DH. In vitro effects of a sulfonylurea on insulin action in adipocytes. Potentiation of insulin-stimulated hexose transport. J Clin Invest. 1981 Jul;68(1):85-90

[5]Cortes P, Riser BL, Asano K, Rodríguez-Barbero A, Narins RG, Yee J. Effects of oral antihyperglycemic agents on extracellular matrix synthesis by mesangial cells. Kidney Int. 1998 Dec;54(6):1985-98