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/ Tolbutamide

甲苯磺丁脲 /Tolbutamide {[allProObj[0].p_purity_real_show]}

货号：A315619 同义名： D 860;HLS 831

Tolbutamide is a potassium channel blocker, sulfonylurea oral hypoglycemic drug.

Tolbutamide 化学结构 CAS号：64-77-7
Tolbutamide 化学结构
CAS号：64-77-7
Tolbutamide 3D分子结构
CAS号：64-77-7
Tolbutamide 化学结构 CAS号：64-77-7
Tolbutamide 3D分子结构 CAS号：64-77-7
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Tolbutamide 纯度/质量文件 产品仅供科研

货号：A315619 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Potassium Channel ↓ 其他靶点 纯度
Tolbutamide ✔ 98%
Glimepiride ++++

SUR2B, IC50: 7.3 nM

SUR1, IC50: 5.4 nM

 		97%
Dronedarone Hydrochloride ✔ 95%
Gliquidone ++

Potassium channel, IC50: 27.2 nM

 		98%
TRAM-34 +++

IKCa1 (KCa3.1), Kd: 20 nM

 		98%
Glibenclamide ✔ 98%
Amiodarone HCl ✔ 97%
Gliclazide ++

Potassium channel, IC50: 184 nM

 		98%
Repaglinide ✔ 98%
Dofetilide ✔ 98%
Nateglinide ✔ 99%
Quinine hydrochloride dihydrate ✔ 98%
ML133 HCl +

Kir2.1, IC50: 290 nM

 		97%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Tolbutamide 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].

Tolbutamide 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 <<

Tolbutamide 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

Tolbutamide 实验方案

计算器
存储液制备 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

Tolbutamide 技术信息

CAS号64-77-7
分子式C12H18N2O3S
分子量 270.35
别名 D 860;HLS 831;Tolbutamide, Artosin, Diabetol, Orinase;U-2043;NSC 87833;NSC 23813
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Room Temperature
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

Tags: Tolbutamide | D 860;HLS 831;Tolbutamide, Artosin, Diabetol, Orinase;U-2043;NSC 87833;NSC 23813 | Drug Standard | Potassium Channel | AmBeed-信号通路专用抑制剂 | Tolbutamide 纯度/质量文件 | Tolbutamide 亚型比较 | Tolbutamide 生物活性 | Tolbutamide 临床数据 | Tolbutamide 参考文献 | Tolbutamide 实验方案 | Tolbutamide 技术信息

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