Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Lubiprostone (RU-0211) 是一种 ClC-2 氯化物通道的激活剂,用于治疗特发性慢性便秘。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 228 | 现货 | ||
2 mg | ¥ 329 | 现货 | ||
5 mg | ¥ 578 | 现货 | ||
10 mg | ¥ 913 | 现货 | ||
25 mg | ¥ 1,770 | 现货 | ||
50 mg | ¥ 3,230 | 现货 | ||
100 mg | ¥ 4,780 | 现货 | ||
500 mg | ¥ 9,870 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 638 | 现货 |
产品描述 | Lubiprostone (RU-0211), an activator of ClC-2 chloride channels, is used in the therapy of idiopathic chronic constipation. |
体外活性 | Lubiprostone induces a robust secretory response in T84 monolayers. Lubiprostone induces a rise in cAMP levels that was sensitive to EP(4)-receptor blockage in T84 cells. [1] Lubiprostone induces a contraction in rat and human stomach longitudinal muscle, which is inhibited by pretreatment with the EP(1) receptor antagonist but not by the EP(3) or EP(4) receptor antagonists. Lubiprostone also reduces electrically stimulated, neuronal contractions in rat and human colon circular muscle preparations. [2] Lubiprostone (1 mM) stimulates higher elevations in TER despite lower I(sc) responses compared with the nonselective secretory agonist PGE(2) (1 mM). Lubiprostone significantly reduces mucosal-to-serosal fluxes of (3)H-labeled mannitol to levels comparable to those of normal control tissues and restored occludin localization to tight junctions. [3] Lubiprostone causes comparable and maximal increases of I(sc) in T84 cells. Lubiprostone-induced increases in iodide efflux are ~80% of those obtained with forskolin. Lubiprostone activates Cl(-) secretion in T84 cells via cAMP, protein kinase A, and by increasing apical membrane CFTR protein. [4] Lubiprostone, applied to the small intestinal mucosa in eight concentrations ranging from 1-3000 nM, evokes increases in Isc in a concentration-dependent manner with an EC50 of 42.5 nM. Lubiprostone applied to the mucosa of the colon in eight concentrations ranging from 1-3000 nM evokes increases in Isc in a concentration-dependent manner with an EC50 of 31.7 nM. [5] |
体内活性 | Lubiprostone induces a CdCl(2)-insensitive secretory response in mouse intestine, but fail to induce intestinal Cl(-) secretion in Cftr-null mice. [1] |
激酶实验 | Fluorescence polarization-based competition assay: Inhibition constants ( Ki ) for the antagonists are determined by addition of the IAP protein constructs to wells containing serial dilutions of the antagonists or the peptide AVPW, and the Hid-FAM probe or AVP-diPhe-FAM probe, as appropriate, in the polarization buffer. Samples are read after a 30-minute incubation. Fluorescence polarization values are plotted as a function of the antagonist concentration, and the IC50 values are obtained by fitting the data to a 4-parameter equation using software. Ki values for the antagonists are determined from the IC50 valued. |
别名 | 芦比前列酮, SPI-0211, RU-0211, 鲁比前列酮 |
分子量 | 390.46 |
分子式 | C20H32F2O5 |
CAS No. | 136790-76-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 72 mg/mL (184.4 mM)
DMSO: 72 mg/mL (184.4 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.5611 mL | 12.8054 mL | 25.6108 mL | 64.027 mL |
5 mM | 0.5122 mL | 2.5611 mL | 5.1222 mL | 12.8054 mL | |
10 mM | 0.2561 mL | 1.2805 mL | 2.5611 mL | 6.4027 mL | |
20 mM | 0.1281 mL | 0.6403 mL | 1.2805 mL | 3.2014 mL | |
50 mM | 0.0512 mL | 0.2561 mL | 0.5122 mL | 1.2805 mL | |
100 mM | 0.0256 mL | 0.1281 mL | 0.2561 mL | 0.6403 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Lubiprostone 136790-76-6 Membrane transporter/Ion channel Chloride channel SPI 0211 芦比前列酮 inhibit RU0211 Cl? Channels Inhibitor SPI-0211 Chloride Channel RU-0211 RU 0211 鲁比前列酮 SPI0211 inhibitor