所有图片(1)
别名:
N-Ethyl-carbamic acid 1-(6,7-dimethoxy-1-phthalazinyl)-4-piperidinyl ester, UK 31557
经验公式（希尔记法）:
C18H24N4O4
推荐产品
质量水平
检测方案
≥95% (HPLC)
形式
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
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.
警示用语：
Danger
危险声明
危险分类
Acute Tox. 3 Oral
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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
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
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
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
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.
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 nucleotides like cAMP modulate cell function via PKA activation and ion channels.
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