| Bioactivity | 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]. | ||||||||||||
| Target | β/α-1 adrenergic receptorIC50: 5 μM (lipid peroxidation)Autophagy | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | Carvedilol | ||||||||||||
| CAS | 72956-09-3 | ||||||||||||
| Formula | C24H26N2O4 | ||||||||||||
| Molar Mass | 406.47 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |