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Carvedilol Sale

(Synonyms: 卡维地洛; BM 14190) 目录号 : GC14769

A β-adrenergic receptor antagonist

Carvedilol Chemical Structure

Cas No.:72956-09-3

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥399.00
现货
5g
¥704.00
现货
25g
¥2,531.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Cell experiment [1]:

Cell lines

human neutrophils

Preparation method

The solubility of this compound in DMSO is >20.3mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

10~100μM

Applications

Carvedilol inhibited PMA-induced O2- production in human neutrophils in a dose-dependent manner with an IC50 value of 28μM.

Animal experiment [2]:

Animal models

Lewis rats induced with acute experimental autoimmune myocarditis

Dosage form

20 mg/kg/day for 3 wk

Application

Carvedilol suppressed left ventricular fractional shortening and decreased heart rates, markedly reduced the severity of myocarditis and suppressed thickening of the left ventricular posterior wall in rats with experimental autoimmune myocarditis.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

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.

产品描述

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

Cas No. 72956-09-3 SDF
别名 卡维地洛; BM 14190
化学名 1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)ethylamino]propan-2-ol
Canonical SMILES COC1=CC=CC=C1OCCNCC(COC2=CC=CC3=C2C4=CC=CC=C4N3)O
分子式 C24H26N2O4 分子量 406.47
溶解度 ≥ 40.6mg/mL in DMSO 储存条件 Store at RT
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

制备储备液
1 mg 5 mg 10 mg
1 mM 2.4602 mL 12.301 mL 24.6021 mL
5 mM 0.492 mL 2.4602 mL 4.9204 mL
10 mM 0.246 mL 1.2301 mL 2.4602 mL
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