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Principaux documents

SML0308

Sigma-Aldrich

Carbazeran

≥95% (HPLC)

Synonyme(s) :

N-Ethyl-carbamic acid 1-(6,7-dimethoxy-1-phthalazinyl)-4-piperidinyl ester, UK 31557

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About This Item

Formule empirique (notation de Hill):
C18H24N4O4
Numéro CAS:
Poids moléculaire :
360.41
Numéro MDL:
Code UNSPSC :
41106305
ID de substance PubChem :
Nomenclature NACRES :
NA.77
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Niveau de qualité

Essai

≥95% (HPLC)

Forme

powder

Conditions de stockage

desiccated

Couleur

white to beige

Solubilité

DMSO: ≥2 mg/mL at warmed

Température de stockage

2-8°C

Chaîne SMILES 

CCNC(=O)OC1CCN(CC1)c2nncc3cc(OC)c(OC)cc23

InChI

1S/C18H24N4O4/c1-4-19-18(23)26-13-5-7-22(8-6-13)17-14-10-16(25-3)15(24-2)9-12(14)11-20-21-17/h9-11,13H,4-8H2,1-3H3,(H,19,23)

Clé InChI

QJGVXJYGDBSPSJ-UHFFFAOYSA-N

Description générale

Carbazeran is usedin the treatment of heart failure.[1]

Actions biochimiques/physiologiques

Aldehyde oxidase (AO) substrate; inotropic agent and phosphodiesterase inhibitor
Carbazeran is an Aldehyde oxidase (AO) substrate and a phosphodiesterase inhibitor that produces concentration-dependent positive inotropic responses. In humans, the compound is almost completely cleared via 4-hydroxylation to the phthalazinone metabolite by AO.

Caractéristiques et avantages

This compound is a featured product for Cyclic Nucleotide research. Click here to discover more featured Cyclic Nucleotide products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

Pictogrammes

Skull and crossbones

Mention d'avertissement

Danger

Mentions de danger

Classification des risques

Acute Tox. 3 Oral

Code de la classe de stockage

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable


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Consulter la Bibliothèque de documents

Raman Sharma et al.
Drug metabolism and disposition: the biological fate of chemicals, 40(3), 625-634 (2011-12-23)
The pharmacokinetic properties of drugs may be altered by kinetic deuterium isotope effects. With specifically deuterated model substrates and drugs metabolized by aldehyde oxidase, we demonstrate how knowledge of the enzyme's reaction mechanism, species differences in the role played by
Phosphodiesterase inhibitors: haemodynamic effects related to the treatment of cardiac failure.
W S Hillis et al.
European heart journal, 3 Suppl D, 97-101 (1982-12-01)
B Kaye et al.
Xenobiotica; the fate of foreign compounds in biological systems, 15(3), 237-242 (1985-03-01)
The metabolism of carbazeran has been investigated in vitro using liver cytosol from dog, baboon and man. Carbazeran was not metabolized in cytosol prepared from dog liver but was rapidly metabolized to a single product in baboon- and human-liver cytosol.
David J Wilkinson et al.
The AAPS journal, 19(4), 1163-1174 (2017-05-06)
The importance of aldehyde oxidase (AOX) is becoming increasingly recognized in the prediction of human pharmacokinetic parameters from animal data. The objectives of these studies were to ascertain whether an in vitro-in vivo correlation existed in the clearance and metabolic
B Price et al.
Biochemical pharmacology, 36(23), 4047-4054 (1987-12-01)
Extraction of frozen canine cardiac muscle rendered soluble over 90% of the cyclic AMP phosphodiesterase activity. The residual activity was membrane-bound. Ion exchange chromatography of the soluble activity on DE-52 allowed for the resolution of three distinct cyclic AMP phosphodiesterase

Articles

Cyclic nucleotide phosphodiesterases (PDEs) catalyze the hydrolysis of cAMP and/or cGMP. There are 11 different mammalian PDE families.

Cyclic nucleotide phosphodiesterases (PDEs) catalyze the hydrolysis of cAMP and/or cGMP. There are 11 different mammalian PDE families.

Cyclic nucleotide phosphodiesterases (PDEs) catalyze the hydrolysis of cAMP and/or cGMP. There are 11 different mammalian PDE families.

Cyclic nucleotide phosphodiesterases (PDEs) catalyze the hydrolysis of cAMP and/or cGMP. There are 11 different mammalian PDE families.

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