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Key Documents

492030

Sigma-Aldrich

NS 2028

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

Synonyme(s) :

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

Formule empirique (notation de Hill):
C9H5BrN2O3
Numéro CAS:
Poids moléculaire :
269.05
Numéro MDL:
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

Niveau de qualité

Pureté

≥98% (NMR)

Forme

solid

Fabricant/nom de marque

Calbiochem®

Conditions de stockage

OK to freeze
desiccated

Couleur

white to off-white

Solubilité

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

Conditions d'expédition

ambient

Température de stockage

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

Clé InChI

MUDRLQRJCGJJTB-UHFFFAOYSA-N

Description générale

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).

Actions biochimiques/physiologiques

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

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

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.

Autres remarques

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

Informations légales

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

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable


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Consulter la Bibliothèque de documents

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

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