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Carvedilol

现货
Catalog No.
B1332
强效β-肾上腺素受体和α1-肾上腺素受体拮抗剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 550.00
现货
5g
¥ 910.00
现货
25g
¥ 3,330.00
现货

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Background

Carvedilol(BM14190), an antagonist ofα1- and β-adrenergic receptors (ARs), is used to treat congestive heart failure (CHF) and high blood pressure [1].

Adrenergic receptors, a class of G protein-coupled receptors, are targets of thenorepinephrine and epinephrine which have been involved in sympathetic nervous system[2]..

In vitro: Carvedilol potently inhibited Fe2+-initiated lipid peroxidation in rat brain homogenate with an IC50 of 8.1 μM. In rat brain homogenate, carvedilol protected against Fe2+-induced α-tocopherol depletion with an IC50 of 17.6 μM. Carvedilol dose-dependently decreased the intensity of the DMPO-OH signal, with an IC50 of 25 μM [1]. Carvedilol prevented vascular smooth muscle cell migration, proliferation, and neointimal formation following vascular injury. In human cultured pulmonary artery vascular smooth muscle cells, carvedilol (0.1-10 μM) concentration-dependently inhibited the mitogenesis stimulated by platelet-derived growth factor, epidermal growth factor, thrombin, and serum, with IC50 values ranging from 0.3 to 2.0 μM. Carvedilol concentration-dependently inhibited vascular smooth muscle cell migration induced by platelet-derived growth factor with an IC50 value of 3 μM [3].

References:

[1]. Yue T L, Cheng H Y, Lysko P G, et al. Carvedilol, a new vasodilator and beta adrenoceptor antagonist, is an antioxidant and free radical scavenger[J]. Journal of Pharmacology and Experimental Therapeutics, 1992, 263(1): 92-98.

[2].Furchgott R F. The receptors for epinephrine and norepinephrine (adrenergic receptors)[J]. Pharmacological reviews, 1959, 11(2): 429-441.

[3].Ohlstein E H, Douglas S A, Sung C P, et al. Carvedilol, a cardiovascular drug, prevents vascular smooth muscle cell proliferation, migration, and neointimal formation following vascular injury[J]. Proceedings of the National Academy of Sciences, 1993, 90(13): 6189-6193

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Chemical Properties

StorageStore at -20°C
M.Wt406.47
Cas No.72956-09-3
FormulaC24H26N2O4
Solubility≥40.6mg/mL in DMSO
Chemical Name1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)ethylamino]propan-2-ol
SDFDownload SDF
Canonical SMILESCOC1=CC=CC=C1OCCNCC(COC2=CC=CC3=C2C4=CC=CC=C4N3)O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

人嗜中性粒细胞

溶解方法

在DMSO中的溶解度> 20.3mg/mL。为了获得更高浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

10~100μM

应用

Carvedilol以剂量依赖的方式抑制人中性粒细胞中PMA诱导的O2-产生,IC50值为28μM。

动物实验[2]:

动物模型

诱发急性实验性自身免疫性心肌炎的Lewis大鼠

剂量

20 mg/kg/day,持续3周

应用

Carvedilol可抑制左心室分数缩短,降低心率,明显降低心肌炎的严重程度,抑制实验性自身免疫性心肌炎大鼠左室后壁增厚。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1] Wu TC, Chen YH, Leu HB, Chen YL, Lin FY, Lin SJ, Chen JW. Carvedilol, a pharmacological antioxidant, inhibits neointimal matrix metalloproteinase-2 and -9 in experimental atherosclerosis. Free Radic Biol Med. 2007 Dec 1;43(11):1508-22.

[2] Yuan Z, Shioji K, Kihara Y, Takenaka H, Onozawa Y, Kishimoto C. Cardioprotective effects of carvedilol on acute autoimmune myocarditis: anti-inflammatory effects associated with antioxidant property. Am J Physiol Heart Circ Physiol. 2004 Jan;286(1):H83-90.

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