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SML0308

Carbazeran

≥95% (HPLC), Aldehyde oxidase (AO) substrate, powder

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):
C18H24N4O4
CAS Number:
Molecular Weight:
360.41
UNSPSC Code:
41106305
PubChem Substance ID:
NACRES:
NA.77
MDL number:
Assay:
≥95% (HPLC)
Form:
powder
Quality level:
Storage condition:
desiccated
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Product Name

Carbazeran, ≥95% (HPLC)

Quality Level

assay

≥95% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

DMSO: ≥2 mg/mL at warmed

storage temp.

2-8°C

SMILES string

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)

InChI key

QJGVXJYGDBSPSJ-UHFFFAOYSA-N

General description

Carbazeran is usedin the treatment of heart failure.

Biochem/physiol Actions

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.

Features and Benefits

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.

pictograms

Skull and crossbones

signalword

Danger

hcodes

Hazard Classifications

Acute Tox. 3 Oral

Storage Class

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

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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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.
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)
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
C R Taylor et al.
American heart journal, 102(3 Pt 2), 515-532 (1981-09-01)
The animal and human pharmacology of several new drugs (prazosin, trimazosin, pirbuterol, and carbazeran) useful in the treatment of congestive heart failure (CHF) is delineated in relation to the pharmacology of other agents employed for CHF management. Prazosin and trimazosin
Drug Metabolism: Towards the Next Millennium, 45-45 (1998)

Articles

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

Cyclic nucleotides like cAMP modulate cell function via PKA activation and ion channels.

环核苷酸磷酸二酯酶 (PDEs) 催化 cAMP 和/或 cGMP 的水解。存在有11种不同的哺乳动物PDE家族。

Global Trade Item Number

SKUGTIN
SML0308-5MG04061832899633
SML0308-25MG04061832899626

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