详细介绍

Carvedilol (Synonyms: 卡维-地洛）

生物活性

Carvedilol (BM 14190) is a non-selective β/α-1 blocker^[1]. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC₅₀ of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure^[2]. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome^[3].

IC₅₀ & Target

β/α-1 adrenergic receptor^[1]
IC50: 5 μM (lipid peroxidation)^[2]
Autophagy^[3]

体外研究(In Vitro)

Superoxide generation by activated human neutrophils in vitro is inhibited by Carvedilol with an IC₅₀ of 28 μM. Carvedilol is shown to scavenge oxygen free radicals in a cell-free system with an IC₅₀ of 25 μM^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量：406.47

Formula：C₂₄H₂₆N₂O₄

CAS 号：72956-09-3

中文名称：卡维-地洛；卡维地罗

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 100 mg/mL (246.02 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4602 mL	12.3010 mL	24.6021 mL
5 mM	0.4920 mL	2.4602 mL	4.9204 mL
10 mM	0.2460 mL	1.2301 mL	2.4602 mL

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, 6 months; -20°C, 1 month。-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。

In Vivo:

以下溶解方案都请先按照 In Vitro 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，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制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

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (6.15 mM); Clear solution
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (6.15 mM); Suspended solution; Need ultrasonic
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.15 mM); Clear solution

参考文献

[1]. Eggertsen R, et al. Acute haemodynamic effects of carvedilol (BM 14190), a new combined beta-adrenoceptor blocker and precapillary vasodilating agent, in hypertensive patients. Eur J Clin Pharmacol. 1984;27(1):19-22.

[2]. Feuerstein GZ, et al. Myocardial protection by the novel vasodilating beta-blocker, carvedilol: potential relevance of anti-oxidant activity. J Hypertens Suppl. 1993 Jun;11(4):S41-8.

[3]. Wong WT, et al. Repositioning of the β-Blocker Carvedilol as a Novel Autophagy Inducer That Inhibits the NLRP3 Inflammasome. Front Immunol. 2018 Aug 22;9:1920.

注：产品仅用于科研

产品简介

详细介绍

Carvedilol (Synonyms: 卡维-地洛）