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SML0308

Sigma-Aldrich

Carbazeran

≥95% (HPLC)

别名:

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

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About This Item

经验公式（希尔记法）:
C18H24N4O4
CAS号:
70724-25-3
分子量:
360.41
MDL编号:
MFCD00867107
UNSPSC代码:
41106305
PubChem化学物质编号:
329825313
NACRES:
NA.77

质量水平

100

方案

≥95% (HPLC)

表单

powder

储存条件

desiccated

颜色

white to beige

溶解性

DMSO: ≥2 mg/mL at warmed

储存温度

2-8°C

SMILES字符串

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

一般描述

Carbazeran is usedin the treatment of heart failure.

生化/生理作用

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.

特点和优势

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.

象形图

Skull and crossbones
GHS06

警示用语：

Danger

危险声明

H301

危险分类

Acute Tox. 3 Oral

储存分类代码

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

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000202711
0000185948
0000185949
0000156762
0000156761

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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
T Eric Ballard et al.
Drug metabolism and disposition: the biological fate of chemicals, 44(2), 172-179 (2015-11-27)
Laboratory animal models are the industry standard for preclinical risk assessment of drug candidates. Thus, it is important that these species possess profiles of drug metabolites that are similar to those anticipated in human, since metabolites also could be responsible
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
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