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Merck
CN

492030

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
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
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产品名称

NS 2028, Potent, specific, and irreversible inhibitor of soluble guanylyl cyclase.

SMILES string

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

assay

≥98% (NMR)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
desiccated

color

white to off-white

solubility

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

shipped in

ambient

storage temp.

2-8°C

Quality Level

Biochem/physiol Actions

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

Disclaimer

Toxicity: Standard Handling (A)

General description

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).

Other Notes

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

Preparation Note

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.

Legal Information

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

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_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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