(±)-柚皮素 TMS2171

Product Introduction
Bioactivity


英文名: (±)-Naringenin

描述: (±)-Naringenin (Naringenine) 是一种天然的类黄酮。它通过激活肌细胞中 BKCa 通道发挥对内皮剥脱血管的舒张作用。

细胞实验: Naringenin is dissolved in DMSO and diluted in cell culture medium. The cells are rinsed with PBS and grown in a medium containing various concentrations of naringenin (50, 100, 150, 200, 250, 300 μM). The solvent DMSO treated cells are served as control. After 24 hrs of treatment, the medium is removed and replaced by another medium containing MTT. Cell viability is measured using the MTT assay[1].

体内活性: (+/-)-Naringenin induced concentration-dependent relaxation in endothelium-denuded rat aortic rings pre-contracted with either 20 mM KCl or noradrenaline (pIC(50) values of 4.74 and 4.68, respectively).?Tetraethylammonium, iberiotoxin, 4-aminopyridine and 60 mM KCl antagonised (+/-)-naringenin-induced vasorelaxation, while glibenclamide did not produce any significant antagonism.?Naringin [(+/-)-naringenin 7-beta-neohesperidoside] caused a concentration-dependent relaxation of rings pre-contracted with 20 mM KCl, although its potency and efficacy were significantly lower than those of (+/-)-naringenin.?In rat tail artery myocytes, (+/-)-naringenin increased large conductance Ca(2+)-activated K(+) (BK(Ca)) currents in a concentration-dependent manner;?this stimulation was iberiotoxin-sensitive and fully reversible upon drug wash-out.?(+/-)-Naringenin accelerated the activation kinetics of BK(Ca) current, shifted, by 22 mV, the voltage dependence of the activation curve to more negative potentials, and decreased the slope of activation.?(+/-)-Naringenin-induced stimulation of BK(Ca) current was insensitive either to changes in the intracellular Ca(2+) concentration or to the presence, in the pipette solution, of the fast Ca(2+) chelator BAPTA.?However, such stimulation was diminished when the K(+) gradient across the membrane was reduced.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : < 0.1 mg/mL (insoluble)
DMSO : 60 mg/mL (220.39 mM)


关键字: Potassium Channel | inhibit | (±)Naringenin | (±)-Naringenin | myocytes | vasorelaxant | (±) Naringenin | Inhibitor | KcsA

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相关库: PBCRBS Traditional Chinese Medicine Compound Library | Anti-Cancer Compound Library | Polyphenolic Natural Product Library | Selected Plant-Sourced Compound Library | Membrane Protein-targeted Compound Library | Chinese Pharmacopoeia Natural Product Library | Traditional Chinese Medicine Monomer Library | Tibetan medicine Compound Library | NO PAINS Compound Library | Bioactive Compound Library

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