A β-adrenergic receptor antagonist
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Carvedilol

Item No. 15418

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-(9H-carbazol-4-yloxy)-3-[[2-(2-methoxyphenoxy)ethyl]amino]-2-propanol
CAS Number
72956-09-3
Synonyms
  • BM 14190
Molecular Formula
C24H26N2O4
Formula Weight
406.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:4): 0.2 mg/mlEthanol: 5 mg/ml
λmax
224, 243, 286, 321, 333 nm
SMILES
COC1=C(OCCNCC(COC2=C(C(C=CC=C3)=C3N4)C4=CC=C2)O)C=CC=C1
InChi Code
InChI=1S/C24H26N2O4/c1-28-21-10-4-5-11-22(21)29-14-13-25-15-17(27)16-30-23-12-6-9-20-24(23)18-7-2-3-8-19(18)26-20/h2-12,17,25-27H,13-16H2,1H3
InChi Key
OGHNVEJMJSYVRP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Cayman Chemical
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    Product Description

    Carvedilol is an antagonist of the β-adrenergic receptor (β-AR; Kds = 1.78, 0.4, and 5.01 nM for β1-, β2-, and β3-ARs, respectively).1 It also selectively binds to α1- over α2-ARs (Kis = 0.81 and 3,400 nM, respectively).2 Carvedilol reverses increases in heart rate induced by the β1-AR agonist isoproterenol (Item No. 15592) in isolated guinea pig atria (Kb = 0.8 nM).3 It prevents epinephrine-induced premature ventricular beats in a rat model of arrhythmia with an ED50 value of 0.25 mg/kg.2 Carvedilol inhibits the contractile response to the α1-AR agonist norepinephrine in isolated rabbit aorta (Kb = 11 nM).3 It decreases systolic blood pressure and heart rate in rat models of hypertension, including spontaneously hypertensive, renal hypertensive, and DOCA-salt hypertensive rats when administered at doses ranging from 3 to 30 mg/kg, as well as activates cardioprotective signaling through β-arrestin and ERK1/2 activation.4,5,6,7 Carvedilol also inhibits severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (Mpro), also known as 3C-like protease (3CLpro; IC50 = 204.6 µg/ml) and reduces viral infectivity in SARS-CoV-2-infected Vero E6 cells (IC50 = 0.350 µg/ml).8 Formulations containing carvedilol have been used in the treatment of congestive heart failure and hypertension.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Baker, J.G. The selectivity of β-adrenoceptor antagonists at the human β1, β2 and β3 adrenoceptors. Br. J. Pharmacol. 144(3), 317-322 (2005).

    2. Groszek, G., Nowak-Król, A., Wdowik, T., et al. Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxy phenoxy)ethylamino)propan-2-ol analogs and its enantiomers. Part 2. Eur. J. Med. Chem. 44(12), 5103-5111 (2009).

    3. Nichols, A.J., Sulpizio, A.C., Ashton, D.J., et al. In vitro pharmacologic profile of the novel beta-adrenoceptor antagonist and vasodilator, carvedilol. Pharmacology 39(5), 327-336 (1989).

    4. Tanaka, M., Masumura, H., Tanaka, S., et al. Studies on the antihypertensive properties of carvedilol, a compound with beta-blocking and vasodilating effects. J. Cardiovasc. Pharmacol. 10(Suppl 11), S52-S57 (1987).

    5. Wisler, J.W., DeWire, S.M., Whalen, E.J., et al. A unique mechanism of β-blocker action: Carvedilol stimulates β-arrestin signaling. Proc. Natl. Acad. Sci. USA 104(42), 16657-16662 (2007).

    6. Kim, I.M., Tilley, D.G., Chen, J., et al. β-blockers alprenolol and carvedilol stimulate β-arrestin-mediated EGFR transactivation. Proc. Natl. Acad. Sci. USA 105(38), 14555-14560 (2008).

    7. Ibrahim, I.A.A.E.H., and Kurose, H. β-Arrestin-mediated signaling improves the efficacy of therapeutics. J. Pharmacol. Sci. 118(4), 408-412 (2012).

    8. Hamed, M.I.A., Darwish, K.M., Soltane, R., et al. β-Blockers bearing hydroxyethylamine and hydroxyethylene as potential SARS-CoV-2 Mpro inhibitors: Rational based design, in silico, in vitro, and SAR studies for lead optimization. RSC Adv. 11(56), 35536-35558 (2021).