Carvedilol

Carvedilol is an antagonist of the beta-adrenergic receptor (beta-AR, Kds = 1.78, 0.4, and 5.01 nM for beta1-, beta2-, and beta3-ARs, respectively). It also selectively binds to alpha1- over alpha2-ARs (Kis = 0.81 and 3,400 nM, respectively). Carvedilol reverses increases in heart rate induced by the beta1-AR agonist isoproterenol (Cay-15592) in isolated guinea pig atria (Kb = 0.8 nM). It prevents epinephrine-induced premature ventricular beats in a rat model of arrhythmia with an ED50 value of 0.25 mg/kg. Carvedilol inhibits the contractile response to the alpha1-AR agonist norepinephrine in isolated rabbit aorta (Kb = 11 nM). 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 beta-arrestin and ERK1/2 activation. 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). Formulations containing carvedilol have been used in the treatment of congestive heart failure and hypertension.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: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:4): 0.2 mg/ml, Ethanol: 5 mg/ml. lambdamax: 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.