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Merck
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Key Documents

SMB00929

Sigma-Aldrich

5′-Hydroxy carvedilol

≥95% (HPLC)

同義詞:

5′-Hydroxy carvedilol, 3-[2-[[3-(9H-Carbazol-4-yloxy)-2-hydroxypropyl]amino]ethoxy]-4-methoxyphenol, 5′-Hydroxyphenyl carvedilol, 5′-Hydroxyphenylcarvedilol, 5′-OH carvedilol, 5-Hydroxycarvedilol, 5OHC, BM-140830, Carvedilol metabolite M5

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About This Item

經驗公式(希爾表示法):
C24H26N2O5
CAS號碼:
分子量::
422.47
分類程式碼代碼:
12352200
NACRES:
NA.25

品質等級

化驗

≥95% (HPLC)

形狀

solid

顏色

off-white

溶解度

DMSO: soluble, clear, colorless

儲存溫度

2-8°C

InChI

1S/C24H26N2O5/c1-29-21-10-9-16(27)13-23(21)30-12-11-25-14-17(28)15-31-22-8-4-7-20-24(22)18-5-2-3-6-19(18)26-20/h2-10,13,17,25-28H,11-12,14-15H2,1H3

InChI 密鑰

PVUVZUBTCLBJMT-UHFFFAOYSA-N

一般說明

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.

其他說明

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象形圖

Health hazardEnvironment

訊號詞

Warning

危險聲明

危險分類

Aquatic Chronic 2 - STOT RE 2

標靶器官

Liver,spleen,Adrenal gland,Uterus (including cervix)

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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分析證明 (COA)

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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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