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首页 / 抑制剂/激动剂 / 膜转运蛋白 / 钾通道 / Tolbutamide/甲苯磺丁脲

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

货号：A315619 同义名： D 860; HLS 831

Tolbutamide是一种口服活性的KATP抑制剂，通过抑制细胞增殖及刺激胰高血糖素分泌，具有降糖作用，主要用于II型糖尿病相关机制的研究。

Tolbutamide/甲苯磺丁脲 化学结构 CAS号：64-77-7
Tolbutamide/甲苯磺丁脲 化学结构
CAS号：64-77-7
Tolbutamide/甲苯磺丁脲 3D分子结构
CAS号：64-77-7
Tolbutamide/甲苯磺丁脲 化学结构 CAS号：64-77-7
Tolbutamide/甲苯磺丁脲 3D分子结构 CAS号：64-77-7
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Tolbutamide/甲苯磺丁脲 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 ++++

SUR1, IC50: 5.4 nM

SUR2B, IC50: 7.3 nM

 		97%
Dronedarone HCl ✔ 95%
Gliquidone ++

Potassium channel, IC50: 27.2 nM

 		99%
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 HCl dihydrate ✔ 98%
ML133 HCl +

Kir2.1, IC50: 290 nM

 		99%
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/甲苯磺丁脲 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/甲苯磺丁脲 细胞实验

Cell Line
Concentration Treated Time Description References
Mouse pancreatic β-cells 5-100 µM 12 minutes Investigate the effect of tolbutamide on cytoplasmic Ca2+ concentration in β-cells, showing that tolbutamide induces a [Ca2+]i rise by closing K+-ATP channels, with response amplitude increasing with drug concentration. Br J Pharmacol. 2001 Jun;133(4):575-85
Freshly-dispersed ventromedial hypothalmic nucleus (VMHN) neurones 0.1-10 mM up to 20 min To test the effects of Tolbutamide on ATP-K+ channel currents, showing no significant inhibition. Br J Pharmacol. 1990 Nov;101(3):531-40

Tolbutamide/甲苯磺丁脲 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Rats Glucoreceptive VMHN neurones in hypothalamic slices Superfusion 0.1 mM Single application, lasting 1 min To test the effects of Tolbutamide on glucoreceptive neurones, showing it depolarized the cells and increased membrane resistance. Br J Pharmacol. 1990 Nov;101(3):531-40
Mice Anesthetized mice Intravenous injection 1800 mg/kg Single injection To study the effect of tolbutamide on the electrical activity of mouse pancreatic β-cells, showing that tolbutamide transformed the oscillatory pattern into continuous electrical activity, associated with a decrease in blood glucose concentration. Br J Pharmacol. 1998 Feb;123(3):443-8
Rats Wistar rats Intravenous injection 50 mg/kg Single dose To study the pharmacokinetic interactions of tolbutamide, including the effects of enzyme induction and inhibition. Results showed that phenobarbitone pretreatment significantly decreased the half-life and AUC of tolbutamide and increased clearance and volume of distribution, while primaquine and cimetidine significantly increased half-life and AUC and decreased clearance. Br J Pharmacol. 1984 Mar;81(3):557-62

Tolbutamide/甲苯磺丁脲 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/甲苯磺丁脲 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/甲苯磺丁脲 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/甲苯磺丁脲 技术信息

CAS号64-77-7
分子式C12H18N2O3S
分子量 270.35
SMILES Code O=S(C1=CC=C(C)C=C1)(NC(NCCCC)=O)=O
MDL No. MFCD00027169
别名 D 860; HLS 831; Tolbutamide, Artosin, Diabetol, Orinase; U-2043; NSC 87833; NSC 23813
运输蓝冰
InChI Key JLRGJRBPOGGCBT-UHFFFAOYSA-N
Pubchem ID 5505
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, room temperature
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三

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/甲苯磺丁脲 纯度/质量文件 | Tolbutamide/甲苯磺丁脲 亚型比较 | Tolbutamide/甲苯磺丁脲 生物活性 | Tolbutamide/甲苯磺丁脲 临床数据 | Tolbutamide/甲苯磺丁脲 参考文献 | Tolbutamide/甲苯磺丁脲 实验方案 | Tolbutamide/甲苯磺丁脲 技术信息

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