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Merck
CN

SML0308

Carbazeran

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

别名:

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

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关于此项目

经验公式（希尔记法）:
C18H24N4O4
化学文摘社编号:
70724-25-3
分子量:
360.41
UNSPSC Code:
41106305
PubChem Substance ID:
329825313
NACRES:
NA.77
MDL number:
MFCD00867107

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产品名称

Carbazeran, ≥95% (HPLC)

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

assay

≥95% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

DMSO: ≥2 mg/mL at warmed

storage temp.

2-8°C

Quality Level

100

相关类别

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.

General description

Carbazeran is usedin the treatment of heart failure.

pictograms

Skull and crossbones
GHS06

signalword

Danger

hcodes

H301

Hazard Classifications

Acute Tox. 3 Oral

存储类别

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

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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Wee Kiat Tan et al.
The Journal of pharmacology and experimental therapeutics, 374(2), 295-307 (2020-05-13)
Gefitinib and erlotinib are epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs) with activity against metastatic non-small cell lung cancer. Aldehyde oxidase-1 (AOX1) is a cytosolic drug-metabolizing enzyme. We conducted an experimental and molecular docking study on the effect of gefitinib
Shotaro Uehara et al.
Drug metabolism and disposition: the biological fate of chemicals, 48(7), 580-586 (2020-05-03)
Carbazeran is a potent phosphodiesterase inhibitor with species-dependent metabolic profiles in rats, dogs, and humans. In this study, we investigated the aldehyde oxidase (AOX)-mediated oxidation of carbazeran to 4-oxo derivatives in chimeric NOD/Shi-scid IL2 receptor gamma-null mice expressing a herpes
D el Allaf et al.
Archives internationales de physiologie et de biochimie, 92(4), S69-S79 (1984-11-01)
Compounds with phosphodiesterase inhibitory activity stimulate myocardial contractility by increasing the intracellular cyclic AMP concentrations. They can also increase Ca2+ entry and inhibit Ca2+ sequestration by the sarcoplasmic reticulum. Xanthines produce bronchodilation with associated venous and arteriolar dilation. However, their
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
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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商品

Phosphodiesterases

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

Discover Bioactive Molecules for Nucleotides

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

磷酸二酯酶类

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。

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