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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEProcion Blue HBCat. No.: HY-D0965CAS No.: 12236-82-7Synonyms: Reactive Blue 2分式: CHClNOS分量: 774.16作靶點(diǎn): Others作通路: Others儲(chǔ)存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO :

2、110 mg/mL (142.09 mM)H2O : 10 mg/mL (12.92 mM; Need ultrasonic)Ethanol : 1 mg/mL (insoluble)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 1.2917 mL 6.4586 mL 12.9172 mL5 mM 0.2583 mL 1.2917 mL 2.5834 mL10 mM 0.1292 mL 0.6459 mL 1.2917 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度,選擇

3、合適的溶劑配制儲(chǔ)備液,并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Procion Blue HB (Reactive Blue 2)是嘌呤能拮抗劑。體外研究Reactive Blue 2 is used as an ATP receptor antagonist and induces Ca2+ oscillations in HeLa cells. ReactiveBlue 2 enhances a Ca2+ response to histamine that is linked to the PLC cascade. Reactive Blue 2 may

4、1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEactivate the PLC cascade in an extracellular Ca2+-dependent manner and induce Ca2+ oscillations 1. Theapplication of Reactive Blue 2 increases K+ secretion in a dose-dependent manner, and this increase ischaracterized as a peak followed by a partial r

5、elaxation to a steady-state. Reactive Blue 2 has antagonisticactivities at P2Y4, and the antagonist potency at P2Y4 paralleled the potency of K+ secretion 2.Theanthraquinone dye reactive blue 2 is found to be a potent inhibitor of a protein kinase isolated and purifiedfrom thylakoids. The mode of in

6、hibition is noncompetitive, with a Ki of 8 M for the membrane-bound kinase,and 6 microM for the purified kinase. The inhibitor does not modify the substrate preference of theendogenous kinase and could be removed from the membrane by washing 3. Reactive blue 2 selectivelyinhibits responses mediated

7、via the P2ypurinoceptor, at least within a limited concentration range. Inpreparations where the tone has been raised with noradrenaline, ATP and 2-methylthio ATP, but not ,-methylene ATP, produce relaxations of the vessel. These relaxations are inhibited in the presence of reactiveblue 2 4. Reactiv

8、e blue 2, at concentrations of 0.3-10 M blocks the ATP-induced oscillation in aconcentration-dependent manner 5.REFERENCES1. Okuda A, et al. Reactive blue 2 induces calcium oscillations in HeLa cells. Jpn J Physiol. 2001 Jun;51(3):389-93.2. Lee JH, et al. Reactive blue 2, an antagonist of rat P2Y4,

9、increases K+ secretion in rat cochlea strial marginal cells. Hear Res. 2006Sep;219(1-2):66-73.3. Coughlan SJ, et al. Reactive blue 2 is a potent inhibitor of a thylakoid protein kinase. Eur J Biochem. 1991 Apr 23;197(2):467-71.4. Burnstock G, et al. P2-purinoceptors of two subtypes in the rabbit mes

10、enteric artery: reactive blue 2 selectively inhibits responsesmediated via the P2y-but not the P2x-purinoceptor. Br J Pharmacol. 1987 Feb;90(2):383-91.5. Uneyama H, et al. Suramin and reactive blue 2 are antagonists for a newly identified purinoceptor on rat megakaryocyte. Br JPharmacol. 1994 Jan;111(1):245-9.McePdfHeightCaution: Product has not been fully val

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