SMB00928

Sigma-Aldrich

4′-Hydroxy carvedilol

Sinónimos:
4-(2-(3-(9H-carbazol-4-yloxy)-2-hydroxypropylamino)ethoxy)-3-methoxyphenol, BM 14686, 4′-OH carvedilol, 4′-Hydroxyphenyl carvedilol, 4′OH-CVD, 4′-Hydroxy carvedilol, 4-[2-[[3-(9H-Carbazol-4-yloxy)-2-hydroxypropyl]amino]ethoxy]-3-methoxyphenol, Carvedilol metabolite M4, BM 140686, 4OHC
Empirical Formula (Hill Notation):
C24H26N2O5
Número de CAS:
Peso molecular:
422.47
En este momento no podemos mostrarle ni los precios ni la disponibilidad

Quality Level

assay

≥95%

form

solid

color

off-white to white

storage temp.

2-8°C

General description

Carvedilol is a β- and α1-adrenoreceptor blocker for the treatment of hypertension and congestive heart failure (CHF). The drug is metabolized by CYP2D6 (to 4′-OH and 5′-OH), CYP2C9 (to O-desmethyl), CYP1A2 (to 8-OH). It is also oxidized to 1-OH carvedilol, but the enzyme involved is not yet clear. These metabolites are useful markers for studying and monitoring the activities of cytochrome metabolizing enzymes. M4 metabolite (4′-OH), but not M2 or M5, is most likely to contribute to total β-adrenoceptor blocking activity due to its higher potency.

Application

Metabolomics

WGK Germany

WGK 3

Certificado de Análisis
W H Schaefer et al.
Drug metabolism and disposition: the biological fate of chemicals, 26(10), 958-969 (1998-10-08)
The excretion and biotransformation of carvedilol [1-[carbazolyl-(4)-oxy]-3-[(2-methoxyphenoxyethyl)amino]-2-p ropanol], a new, multiple-action, neurohormonal antagonist that exhibits the combined pharmacological activities of beta-adrenoreceptor antagonism, vasodilation, and antioxidation, were investigated in dogs, rats, and mice. Carvedilol was absorbed well, and biliary secretion was...
Eben Jung et al.
Journal of Korean medical science, 33(27), e182-e182 (2018-07-03)
Carvedilol is commonly used to treat hypertension as a β- and α1-adrenoreceptor blocker, but it is metabolized by CYP2D6, and CYP2D6*10 allele is dominant in Asian population. The objective of this study was to assess the influence of CYP2D6 polymorphisms...
D Tenero et al.
Journal of clinical pharmacology, 40(8), 844-853 (2000-08-10)
Carvedilol is a relatively new drug with beta- and alpha 1-receptor blocking activity and antioxidant effects recently approved for the treatment of congestive heart failure (CHF). An ascending, multiple-dose study was completed in 20 male patients with stable New York...

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