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Merck
CN

R108

Sigma-Aldrich

Ro 41-0960

solid

别名:

2′-Fluoro-3,4-dihydroxy-5-nitrobenzophenone

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About This Item

经验公式(希尔记法):
C13H8FNO5
分子量:
277.20
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77

表单

solid

质量水平

储存条件

protect from light

颜色

yellow

溶解性

H2O: slightly soluble <0.7 mg/mL
45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: 1.0 mg/mL
ethanol: soluble

储存温度

2-8°C

SMILES字符串

Oc1cc(cc(c1O)[N+]([O-])=O)C(=O)c2ccccc2F

InChI

1S/C13H8FNO5/c14-9-4-2-1-3-8(9)12(17)7-5-10(15(19)20)13(18)11(16)6-7/h1-6,16,18H

InChI key

RQPAUNZYTYHKHA-UHFFFAOYSA-N

基因信息

human ... COMT(1312)

应用

Ro 41-0960 has been used as an inhibitor of catechol-O-methyl-transferase in synaptosome membrane preparations and 3T3-L1 adipocytes. It has also been used as a catechol-O-methyl-transferase inhibitor to treat corpus striatum samples to test its effect on dopamine metabolism.

生化/生理作用

Ro 41-0960 is a specific and synthetic inhibitor of the enzyme catechol-O-methyl-transferase (COMT). It binds to the catalytic site and triggers the inhibition of the methylation property of COMT. Ro 41-0960 is effective on uterine leiomyoma lesions and uterine fibroids.

特点和优势

This compound is featured on the Dopamine and Norepinephrine Metabolism page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

注意

Store tightly sealed at 4 °C, protected from exposure to light.

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

个人防护装备

Eyeshields, Gloves, type N95 (US)

法规信息

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分析证书(COA)

Lot/Batch Number

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M Törnwall et al.
Archives internationales de pharmacodynamie et de therapie, 320, 5-20 (1992-11-01)
The effects of three new catechol O-methyltransferase (COMT) inhibitors (nitecapone, entacapone and Ro 41-0960) were assessed on brain neurochemistry and psychomotor tests in levodopa/carbidopa-treated rats and mice. In neurochemical studies in rats, neither nitecapone (3 mg/kg) nor Ro 41-0960 (3
Thijs Beuming et al.
Nature neuroscience, 11(7), 780-789 (2008-06-24)
Cocaine is a widely abused substance with psychostimulant effects that are attributed to inhibition of the dopamine transporter (DAT). We present molecular models for DAT binding of cocaine and cocaine analogs constructed from the high-resolution structure of the bacterial transporter
Tiffany L Graves et al.
Analytical biochemistry, 373(2), 296-306 (2007-11-22)
A high-throughput, competitive fluorescence polarization immunoassay has been developed for the detection of methyltransferase activity. The assay was designed to detect S-adenosylhomocysteine (AdoHcy), a product of all S-adenosylmethionine (AdoMet)-utilizing methyltransferase reactions. We employed commercially available anti-AdoHcy antibody and fluorescein-AdoHcy conjugate
M Törnwall et al.
Pharmacology & toxicology, 69(1), 64-70 (1991-07-01)
3-Nitropyrocatechols are very potent and selective inhibitors of catechol-O-methyltransferase (COMT). LD50 values of three of these compounds were assessed after intraperitoneal administration with a special emphasis on interactions with drugs increasing catecholaminergic neurotransmission. LD50 values of the inhibitors varied from
Mamoun M Alhamadsheh et al.
Science translational medicine, 3(97), 97ra81-97ra81 (2011-08-26)
A valine-to-isoleucine mutation at position 122 of the serum protein transthyretin (TTR), found in 3 to 4% of African Americans, alters its stability, leading to amyloidogenesis and cardiomyopathy. In addition, 10 to 15% of individuals older than 65 years develop

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