Carvedilol - CAS 72956-09-3
Catalog number:
72956-09-3
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C24H26N2O4
Molecular Weight:
406.47
COA:
Inquire
Targets:
Adrenergic Receptor
Description:
Carvedilol is a non-selective beta blocker/alpha-1 blocker with an IC50 of 3.8 μM for inhibition of LDL oxidation.
Publictions citing BOC Sciences Products
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Purity:
>98%
MSDS:
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1.Anti-Anginal and Metabolic Effects of Carvedilol and Atenolol in Patients with Stable Angina Pectoris: A Prospective, Randomized, Parallel, Open-Label Study.
Oh PC1, Kang WC2, Moon J1, Park YM1, Kim S1, Kim MG1, Lee K1, Ahn T1, Shin EK1. Am J Cardiovasc Drugs. 2016 Mar 28. [Epub ahead of print]
BACKGROUND: While recent guidelines have suggested the potential for beta-blockers as first-line agents in chronic stable angina, few data regarding comparative anti-anginal and metabolic effects between beta-blockers with and without vasodilating properties have been reported, particularly in patients with angina pectoris.
2.Chiral analysis of carvedilol and its metabolites hydroxyphenyl carvedilol and O-desmethyl
Nardotto GH1, Coelho EB2, Marques MP1, Lanchote VL3. J Chromatogr B Analyt Technol Biomed Life Sci. 2016 Mar 15;1015-1016:173-80. doi: 10.1016/j.jchromb.2016.02.028. Epub 2016 Feb 23.
Carvedilol is an antihypertensive drug, which is available in clinical practice as a racemic mixture. (S)-(-)-carvedilol is a β- and α1-adrenergic antagonist, while (R)-(+)-carvedilol only acts as an α1-adrenergic antagonist. Carvedilol is metabolized mainly by glucuronidation and, to a lesser extent, by CYP2D6 to hydroxyphenyl carvedilol (OHC) and by CYP2C9 to O-desmethyl carvedilol (DMC). This study describes the development and validation of a method for the sequential analysis of the enantiomers of carvedilol, OHC and DMC in plasma using a Chirobiotic(®) V chiral-phase column coupled to an LC-MS/MS system. The method was linear in the range of 0.05-100, 0.05-10 and 0.02-10ng/mL for the carvedilol, OHC and DMC enantiomers, respectively. Application of the method to the investigation of a patient with type 2 diabetes mellitus treated with a single oral dose of 25mg racemic carvedilol showed plasma accumulation of the (R)-(+)-carvedilol, (R)-(+)-DMC and (R)-(+)-OHC enantiomers.
3.Capillary electrophoretic enantioseparation of basic drugs using a new single-isomer cyclodextrin derivative and theoretical study of the chiral recognition mechanism.
Liu Y1,2, Deng M1, Yu J1, Jiang Z1, Guo X1. J Sep Sci. 2016 Mar 3. doi: 10.1002/jssc.201501026. [Epub ahead of print]
A novel single-isomer cyclodextrin derivative, heptakis {2,6-di-O-[3-(1,3-dicarboxyl propylamino)-2-hydroxypropyl]}-β-cyclodextrin (glutamic acid-β-cyclodextrin) was synthesized and used as a chiral selector in capillary electrophoresis for the enantioseparation of 12 basic drugs, including terbutaline, clorprenaline, tulobuterol, clenbuterol, procaterol, carvedilol, econazole, miconazole, homatropine methyl bromide, brompheniramine, chlorpheniramine and pheniramine. The primary factors affecting separation efficiency, which include the background electrolyte pH, the concentration of glutamic acid-β-cyclodextrin and phosphate buffer concentration, were investigated. Satisfactory enantioseparations were obtained using an uncoated fused-silica capillary of 50 cm (effective length 40cm) × 50 μm id with 120 mM phosphate buffer (pH 2.5-4.0) containing 0.5-4.5 mM glutamic acid-β-cyclodextrin as background electrolytes. A voltage of 20 KV was applied and the capillary temperature was kept at 20°C.
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CAS 72956-09-3 Carvedilol

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