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Carvedilol-d5, CAS 929106-58-1
Carvedilol-d5, CAS 929106-58-1
Artikelnummer
CAY25218-1
Verpackungseinheit
1 mg
Hersteller
Cayman Chemical
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Formulation: A solid
Formal Name: 1-(9H-carbazol-4-yloxy)-3-[[2-(2-methoxyphenoxy)ethyl]amino]-2-propan-1,1,2,3,3-d5-ol
Purity: ≥99% deuterated forms (d1-d5)
Formula Markup: C24H21D5N2O4
Formula Weight: 411,5
Shelf life (days): 1460
CAS Number: 929106-58-1
Notes: Carvedilol-d5 is intended for use as an internal standard for the quantification of carvedilol (Item No. 15418) by GC- or LC-MS. Carvedilol is a non-selective antagonist of the β-adrenergic receptor (β-AR; Kds = 1.78, 0.4, and 5.01 nM for β1-, β2-, and β3-ARs, respectively).{25151} It also binds to α1-, but not α2-, adrenergic receptors (Kis = 0.81 and 3,400 nM, respectively).{25150} 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) and induces relaxation of isolated precontracted guinea pig trachea (Kb = 1.3 nM).{43226} It prevents epinephrine-induced premature ventricular beats in a rat model of arrhythmia with an ED50 value of 0.25 mg/kg.{25150} Carvedilol also inhibits the contractile response to the α1-AR agonist norepinephrine in isolated rabbit aorta (Kb = 11 nM).{43226} It decreases systolic blood pressure and heart rate in rat models of hypertension, including spontaneously hypertensive, renal hypertensive, and deoxycorticosterone acetate-treated rats when administered at doses ranging from 3 to 30 mg/kg.{43227} Carvedilol also activates cardioprotective signaling through β-arrestin and ERK1/2 activation.{25152,25153,23372} It 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).{64706} 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-propan-1,1,2,3,3-d5-ol
Purity: ≥99% deuterated forms (d1-d5)
Formula Markup: C24H21D5N2O4
Formula Weight: 411,5
Shelf life (days): 1460
CAS Number: 929106-58-1
Notes: Carvedilol-d5 is intended for use as an internal standard for the quantification of carvedilol (Item No. 15418) by GC- or LC-MS. Carvedilol is a non-selective antagonist of the β-adrenergic receptor (β-AR; Kds = 1.78, 0.4, and 5.01 nM for β1-, β2-, and β3-ARs, respectively).{25151} It also binds to α1-, but not α2-, adrenergic receptors (Kis = 0.81 and 3,400 nM, respectively).{25150} 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) and induces relaxation of isolated precontracted guinea pig trachea (Kb = 1.3 nM).{43226} It prevents epinephrine-induced premature ventricular beats in a rat model of arrhythmia with an ED50 value of 0.25 mg/kg.{25150} Carvedilol also inhibits the contractile response to the α1-AR agonist norepinephrine in isolated rabbit aorta (Kb = 11 nM).{43226} It decreases systolic blood pressure and heart rate in rat models of hypertension, including spontaneously hypertensive, renal hypertensive, and deoxycorticosterone acetate-treated rats when administered at doses ranging from 3 to 30 mg/kg.{43227} Carvedilol also activates cardioprotective signaling through β-arrestin and ERK1/2 activation.{25152,25153,23372} It 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).{64706} Formulations containing carvedilol have been used in the treatment of congestive heart failure and hypertension.
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Gernot Ensinger, M.Sc.
Laurent Haze
