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Tolbutamide

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Chemical Structure| 64-77-7 同义名 : D 860;HLS 831;Tolbutamide, Artosin, Diabetol, Orinase;U-2043;NSC 87833;NSC 23813
CAS号 : 64-77-7
货号 : A315619
分子式 : C12H18N2O3S
纯度 : 98%
分子量 : 270.35
MDL号 : MFCD00027169
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: 35 mg/mL(129.46 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
靶点

  • Potassium Channel
描述 Tolbutamide is a first generation potassium channel blocker, sulfonylurea oral hypoglycemic drug. Tolbutamide act by stimulating β cells of the pancreas to release insulin. Tolbutamide belongs to a class of medications called sulfonylureas. Tolbutamide inhibits both the basal and the cyclic AMP-stimulated protein kinase activities and the IC50 of Tolbutamide is 4 mM. Tolbutamide also inhibits both soluble and membrane-bound protein kinase from canine heart. The Tolbutamide inhibition of adipose tissue cyclic AMP-dependent protein kinase is one possible explanation for the antilipolytic effects of this drug[3]. Moreover, tolbutamide and dbcAMP increase the synthesis of the tumor suppressor protein Cx43 and that they decrease the level of Ki-67, a protein expressed when cells are proliferating[4]. Tolbutamide is a substrate to organic anion transporter 2 (OAT2) alone with transporter affinity [Michaelis-Menten constant (Km)] of 19.5 ± 4.3 µM[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

3.70mL

0.74mL

0.37mL

18.49mL

3.70mL

1.85mL

36.99mL

7.40mL

3.70mL
参考文献

[1]Sanchez-Alvarez R, Paino T, et al. Tolbutamide reduces glioma cell proliferation by increasing connexin43, which promotes the up-regulation of p21 and p27 and subsequent changes in retinoblastoma phosphorylation. Glia. 2006 Aug 1;54(2):125-34.

[2]Wray HL, Harris AW. Adenosine 3', 5'-monophosphate-dependent protein kinase in adipose tissue: inhibition by tolbutamide. Biochem Biophys Res Commun. 1973 Jul 2;53(1):291-4.

[3]Wray HL, Harris AW. Adenosine 3', 5'-monophosphate-dependent protein kinase in adipose tissue: inhibition by tolbutamide. Biochem Biophys Res Commun. 1973;53(1):291-294

[4]Sánchez-Alvarez R, Paíno T, Herrero-González S, Medina JM, Tabernero A. Tolbutamide reduces glioma cell proliferation by increasing connexin43, which promotes the up-regulation of p21 and p27 and subsequent changes in retinoblastoma phosphorylation. Glia. 2006;54(2):125-134

[5]Bi YA, Mathialagan S, Tylaska L, et al. Organic Anion Transporter 2 Mediates Hepatic Uptake of Tolbutamide, a CYP2C9 Probe Drug. J Pharmacol Exp Ther. 2018;364(3):390-398