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Merck
CN

492030

Sigma-Aldrich

NS 2028

Potent, specific, and irreversible inhibitor of soluble guanylyl cyclase.

别名:

NS 2028, 4H-8-Bromo-1,2,4-oxadiazolo(3,4-d)benz(b)(1,4)oxazin-1-one

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关于此项目

经验公式(希尔记法):
C9H5BrN2O3
化学文摘社编号:
分子量:
269.05
MDL编号:
UNSPSC代码:
12352200
NACRES:
NA.77
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质量水平

方案

≥98% (NMR)

表单

solid

制造商/商品名称

Calbiochem®

储存条件

OK to freeze
desiccated

颜色

white to off-white

溶解性

chloroform: 1 mg/mL
DMSO: 5 mg/mL
ethanol: 5 mg/mL

运输

ambient

储存温度

2-8°C

SMILES字符串

Brc1cc2c(cc1)OCc3[n]2[c]([o]n3)=O

InChI

1S/C9H5BrN2O3/c10-5-1-2-7-6(3-5)12-8(4-14-7)11-15-9(12)13/h1-3H,4H2

InChI key

MUDRLQRJCGJJTB-UHFFFAOYSA-N

一般描述

Potent, specific, and irreversible inhibitor of soluble guanylyl cyclase (IC50 = 30 nM for basal and 200 nM for NO-stimulated enzyme activity; IC50 = 17 nM for S-nitrosoglutathione-enhanced soluble guanylyl cyclase activity in homogenates of mouse cerebellum).

生化/生理作用

Cell permeable: no
Primary Target
basal soluble guanylyl cyclase
Product does not compete with ATP.
Reversible: no
Target IC50: 30 nM for basal and 200 nM for NO-stimulated enzyme activity; 17 nM for S-nitrosoglutathione-enhanced soluble guanylyl cyclase activity in homogenates of mouse cerebellum

制备说明

Following reconstitution, aliquot and freeze (-20°C) for long-term storage. DMSO stock solutions are stable for up to 1 month at -20°C and for ~8 h at 4°C. Avoid freeze/thaw cycles of solutions.

其他说明

Fleming, I., et al. 1999. Proc. Natl. Acad. Sci. USA 96, 1123.
Olesen, S.P., et al. 1998. Br. J. Pharmacol. 123, 299.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

免责声明

Toxicity: Standard Handling (A)

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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I Fleming et al.
Proceedings of the National Academy of Sciences of the United States of America, 96(3), 1123-1128 (1999-02-03)
Shear stress and tyrosine phosphatase inhibitors have been shown to activate the endothelial NO synthase (eNOS) in a Ca2+/calmodulin-independent manner. We report here that isometric contraction of rabbit aorta activates eNOS by a pharmacologically identical pathway. Endothelium-intact aortic rings were
S P Olesen et al.
British journal of pharmacology, 123(2), 299-309 (1998-03-07)
1 The haeme-containing soluble guanylyl cyclase (alpha1beta1-heterodimer) is a major intracellular receptor and effector for nitric oxide (NO) and carbon monoxide (CO) and mediates many of their biological actions by increasing cyclic GMP. We have synthesized new oxadiazolo-benz-oxazins and have

商品

Discover definitions and uses for irreversible inhibitors including the types of irreversible inhibitors: suicide inhibitors, heavy metal inhibitors, and time-dependent inhibitors.

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