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492030

Sigma-Aldrich

NS 2028

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

Synonym(e):

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

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About This Item

Empirische Formel (Hill-System):
C9H5BrN2O3
CAS-Nummer:
204326-43-2
Molekulargewicht:
269.05
MDL-Nummer:
MFCD01530052
UNSPSC-Code:
12352200
NACRES:
NA.77

Qualitätsniveau

100

Assay

≥98% (NMR)

Form

solid

Hersteller/Markenname

Calbiochem®

Lagerbedingungen

OK to freeze
desiccated

Farbe

white to off-white

Löslichkeit

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

Versandbedingung

ambient

Lagertemp.

2-8°C

InChI

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

InChIKey

MUDRLQRJCGJJTB-UHFFFAOYSA-N

Allgemeine Beschreibung

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).

Biochem./physiol. Wirkung

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

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

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.

Sonstige Hinweise

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

Rechtliche Hinweise

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

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable

Analysenzertifikate (COA)

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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

Artikel

Irreversible Inhibitors

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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