| Identification | Back Directory | [Name]
CARVEDILOL-D5 | [CAS]
929106-58-1 | [Synonyms]
CARVEDILOL-D5
1-(9H-carbazol-4-yloxy)-1,1,2,3,3-pentadeuterio-3-[2-(2-methoxyphenoxy)ethylamino]propan-2-ol
Carvedilol-D5Q: What is
Carvedilol-D5 Q: What is the CAS Number of
Carvedilol-D5 Q: What is the storage condition of
Carvedilol-D5 Q: What are the applications of
Carvedilol-D5 | [Molecular Formula]
C24H21D5N2O4 | [MDL Number]
MFCD08063416 | [MOL File]
929106-58-1.mol | [Molecular Weight]
411.51 |
| Hazard Information | Back Directory | [Description]
Carvedilol-d5 is intended for use as an internal standard for the quantification of carvedilol 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). It also binds to α1-, but not α2-, adrenergic receptors (Kis = 0.81 and 3,400 nM, respectively). Carvedilol reverses increases in heart rate induced by the β1-AR agonist isoproterenol in isolated guinea pig atria (Kb = 0.8 nM) and induces relaxation of isolated precontracted guinea pig trachea (Kb = 1.3 nM). It prevents epinephrine-induced premature ventricular beats in a rat model of arrhythmia with an ED50 value of 0.25 mg/kg. Carvedilol also inhibits the contractile response to the α1-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 deoxycorticosterone acetate-treated rats when administered at doses ranging from 3 to 30 mg/kg. Carvedilol also activates cardioprotective signaling through β-arrestin and ERK1/2 activation. Formulations containing carvedilol have been used in the treatment of congestive heart failure and hypertension. | [Chemical Properties]
White Solid | [Uses]
Carvedilol-d5 is the labelled analog of Carvedilol, a nonselective β-adrenergic blocker with α1-blocking activity. Carvedilol is an antihypertensive used in the treatment of congestive heart failure. | [Uses]
Labeled Carvedilol, intended for use as an internal standard for the quantification of Carvedilol by GC- or LC-mass spectrometry. | [References]
[1] GRA?YNA GROSZEK . 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[J]. European Journal of Medicinal Chemistry, 2009, 44 12: Pages 5103-5111. DOI: 10.1016/j.ejmech.2009.07.012
[2] A J NICHOLS. In vitro pharmacologic profile of the novel beta-adrenoceptor antagonist and vasodilator, carvedilol.[J]. Pharmacology, 1989, 39 5: 327-336. DOI: 10.1159/000138616
[3] M TANAKA. Studies on the antihypertensive properties of carvedilol, a compound with beta-blocking and vasodilating effects.[J]. Journal of Cardiovascular Pharmacology, 1987, 10 Suppl 11: S52-7.
[4] JAMES W WISLER. A unique mechanism of beta-blocker action: carvedilol stimulates beta-arrestin signaling.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2007, 104 42: 16657-16662. DOI: 10.1073/pnas.0707936104
[5] ISLAM A.A.E.-H. IBRAHIM Hitoshi K. β-Arrestin-Mediated Signaling Improves the Efficacy of Therapeutics[J]. Journal of pharmacological sciences, 2012, 118 4: Pages 408-412. DOI: 10.1254/jphs.11r10cp
[6] 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?[J]. RSC Advances, 2021, 56: 35536-35558. DOI: 10.1039/d1ra04820a |
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