| 名稱 | Tolbutamide |
| 描述 | Tolbutamide (HLS 831) is a sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE. |
| 細胞實驗 | 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) |
| 激酶實驗 | 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. |
| 體外活性 | 連續(xù)七天每天450 mg/kg Tolbutamide處理細胞,能夠明顯增加胰島素和脂肪細胞的結合.結合曲線反映了受體位點數(shù)量的增加而非它們的親和力增加.這種效應與對脂肪組織中胰島素增強應答相關.與對照組相比,在有胰島素存在時,用Tolbutamide處理的動物脂肪細胞能夠明顯地將更多的葡萄糖轉化成脂肪.小的劑量下Tolbutamide能夠通過刺激胰島素的分泌產生代謝效應,但這種劑量不能提供更多的胰島素結合位點.胰島素結合位點的增加僅在大劑量的Tolbutamide存在時出現(xiàn),但這種劑量下,會減少胰島素的整體水平,包括胰腺的分泌和血清中胰島素的水平. |
| 體內活性 | Tolbutamide只能幫助機體正常產生胰島素的這類病人來降低血糖。Tolbutamide能同時抑制基底蛋白激酶和環(huán)腺苷酸激活的蛋白激酶活性,IC50濃度為4 mM。Tolbutamide能夠劑量依賴地抑制胰高血糖素誘導的雙功能蛋白的磷酸化。在儲存10（-9）M 胰高血糖素的情況下,加入2 mM Tolbutamide能夠降低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還能夠抑制犬類心臟中游離以及膜結合蛋白酶的活性。對脂肪組織的環(huán)腺苷酸依賴蛋白激酶活性的抑制作用可能是Tolbutamide抗脂解作用的原因。Tolbutamide還能夠通過增加Cx43的濃度來抑制C6膠質細胞的增殖,Cx 43的濃度與Cdk激酶的抑制因子p21和p27上調所引起的pRb磷酸化降低相關。 |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 247.5 mg/mL (915.48 mM), Sonication is recommended.
Ethanol : 50 mg/mL (184.95 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (7.4 mM), Sonication is recommended.
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| 關鍵字 | Tolbutamide | PotassiumChannel | Potassium Channel | KcsA | Inhibitor | inhibit | HLS-831 | HLS831 | Autophagy |
| 相關產品 | Sodium orthovanadate | Guanidine hydrochloride | Naringin | Aceglutamide | Alginic acid | Cysteamine hydrochloride | Hemin | Hydroxychloroquine | Sildenafil citrate | Stavudine | Tamoxifen | Paeonol |
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