ODQ, Free Base **
產品名稱：ODQ, Free Base
產品貨號：LC O-1666
產品規格：1 G
ODQ is a specific inhibitor for soluble guanylyl cyclase (sGC) and is an important pharmacological tool for differentiating cGMP-mediated from cGMP-independent effects, such as those caused by nitric oxide.
ODQ inhibited relaxations induced by histamine, ATP, nitric oxide, the nitric oxide donors S-nitrosoglutathione, S-nitroso-N-acetyl-D,L-penicillamine, and spermine NONOate, as well as the direct sGC-stimulant YC-1 but not relaxations induced by papaverine and atriopeptin II. Feelisch, M., et al. "The Soluble Guanylyl Cyclase Inhibitor 1H-[1,2,4]Oxadiazolo[4,3,-a]quinoxalin-1-one Is a Nonselective Heme Protein Inhibitor of Nitric Oxide Synthase and Other Cytochrome P-450 Enzymes Involved in Nitric Oxide Donor Bioactivation." Mol. Pharmacol. 56: 243-253 (1999).
ODQ decreased the minimum alveolar anesthesia concentration for isoflurane anesthesia in Sprague-Dawley rats but did not affect their arterial blood pressure or heart rate. Cechova, S. and Pajewski, T.N. "The soluble guanylyl cyclase inhibitor ODQ, 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one, dose-dependently reduces the threshold for isoflurane anesthesia in rats." Anesth. Analg. 99: 752-757 (2004).
The effects of both nitric oxide and ODQ on sGC can be inhibited by myoglobin. Nitric oxide and ODQ exert only minor effects in cardiomyocytes where myoglobin is abundant but they show strong effects in aortic tissue where there is very little myoglobin. Wegener, J.W., et al. "Failure of 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one (ODQ) to inhibit soluble guanylyl cyclase in rat ventricular cardiomyocytes." Br. J. Pharmacol. 127: 693-700 (1999).
ODQ inhibited sGC competitively with nitric oxide. The inhibition resulted in an apparently irreversible oxidation of the prosthetic heme group. Schrammel, A., et al. "Characterization of 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one as a heme-site inhibitor of nitric oxide-sensitive guanylyl cyclase." Mol. Pharmacol. 50: 1-5 (1996).
Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO at 50 mg/mL; soluble in ethanol at 2 mg/mL with warming; very poorly soluble in water; maximum solubility in plain water is estimated to be about 50-100 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility. Disposal: A
