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Merck

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:
分子量:
360.41
MDL號碼:
分類程式碼代碼:
41106305
PubChem物質ID:
NACRES:
NA.77

品質等級

化驗

≥95% (HPLC)

形狀

powder

儲存條件

desiccated

顏色

white to beige

溶解度

DMSO: ≥2 mg/mL at warmed

儲存溫度

2-8°C

SMILES 字串

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 密鑰

QJGVXJYGDBSPSJ-UHFFFAOYSA-N

一般說明

Carbazeran is usedin the treatment of heart failure.

生化/生理作用

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.

特點和優勢

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.

象形圖

Skull and crossbones

訊號詞

Danger

危險聲明

危險分類

Acute Tox. 3 Oral

儲存類別代碼

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

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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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
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
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
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
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

商品

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。

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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