甲苯磺丁脲 T1054

Product Introduction
Bioactivity


英文名: Tolbutamide

描述: Tolbutamide (HLS 831) 是一种磺脲类降糖药，作用和用途与氯丙酰胺相似。

细胞实验: C6 glioma cells are incubated in serum-free DMEM at 37 °C for at least 24 hours before each experiment. Tolbutamide (400 μM) is incubated for 24 hours in serum-free medium. Incubations are performed at 37 °C in an atmosphere of 95% air/5% CO2 with 90–95% humidity. (Only for Reference)

激酶实验: cAMP kinase assay: Diced epididymal fat pads from fed Wistar rats (175-225 gm) are obtained after decapitation and incubated at 37 °C for two hours in Krebs-bicarbonate buffer containing 1.27 mM CaCl2. When added, Tolbutamide is present only during the incubation. After incubation fat pads are rinsed and sonicated in cold Krebs-bicarbonate buffer. The aqueous supematants from centrifugation at 50,000 × g for 30 minutes at 4 °C contained 0.75 to 1.25 mg protein per mL and are assayed for cyclic AMP-stimulated protein kinase activity. The assay is performed in 0.2 mL with these additions, 10 μmoles sodium glycerofiosphate pH 7.0, 2 μmoles sodium fluoride, 0.4 μmoles theophylline, 0.1 μmoles ethylene glyool bis (β-aminoethyl ether)-N, N'-tetraaoetic acid, 3 μmoles magnesium chloride, 0.3 mg mixed histone, 2 nmoles (γ- 32P) ATP, 1 nmoles cyclic AMP when indicated, and 0.05 ml of supernatant.

体外活性: 连续七天每天450 mg/kg Tolbutamide处理细胞,能够明显增加胰岛素和脂肪细胞的结合.结合曲线反映了受体位点数量的增加而非它们的亲和力增加.这种效应与对脂肪组织中胰岛素增强应答相关.与对照组相比,在有胰岛素存在时,用Tolbutamide处理的动物脂肪细胞能够明显地将更多的葡萄糖转化成脂肪.小的剂量下Tolbutamide能够通过刺激胰岛素的分泌产生代谢效应,但这种剂量不能提供更多的胰岛素结合位点.胰岛素结合位点的增加仅在大剂量的Tolbutamide存在时出现,但这种剂量下,会减少胰岛素的整体水平,包括胰腺的分泌和血清中胰岛素的水平.

体内活性: Tolbutamide只能帮助机体正常产生胰岛素的这类病人来降低血糖。Tolbutamide能同时抑制基底蛋白激酶和环腺苷酸激活的蛋白激酶活性,IC50浓度为4 mM。Tolbutamide能够剂量依赖地抑制胰高血糖素诱导的双功能蛋白的磷酸化。在储存10（-9）M 胰高血糖素的情况下,加入2 mM Tolbutamide能够降低6磷酸果糖激酶的活性并增加果糖2,6二磷酸酯酶的活性。Tolbutamide还能够抑制犬类心脏中游离以及膜结合蛋白酶的活性。对脂肪组织的环腺苷酸依赖蛋白激酶活性的抑制作用可能是Tolbutamide抗脂解作用的原因。Tolbutamide还能够通过增加Cx43的浓度来抑制C6胶质细胞的增殖,Cx 43的浓度与Cdk激酶的抑制因子p21和p27上调所引起的pRb磷酸化降低相关。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 60 mg/mL (221.93 mM)
Ethanol : 50 mg/mL (184.9 mM)


关键字: Potassium Channel | inhibit | Inhibitor | Tolbutamide | HLS-831 | KcsA | Autophagy | HLS831

相关产品: Strictosamide | GW9508 | RU-TRAAK-2 | Paederosidic acid methyl ester | Hemitoxin | Maralixibat Chloride | Tipepidine hydrochloride | AmmTX3 TFA | Reserpine | Jingzhaotoxin-XII

相关库: Anti-Aging Compound Library | FDA-Approved Drug Library | Drug Repurposing Compound Library | Potassium Channel Blocker Library | Anti-Cancer Drug Library | Clinical Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Approved Drug Library | Orally Active Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途