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/ Lubiprostone/鲁比前列素

Lubiprostone/鲁比前列素 {[allProObj[0].p_purity_real_show]}

货号：A126294 同义名： 鲁比前列酮 / SPI-0211; RU-0211

Lubiprostone是一种 ClC-2 氯离子通道激活剂，用于特发性慢性便秘的研究。

Lubiprostone/鲁比前列素 化学结构 CAS号：136790-76-6
Lubiprostone/鲁比前列素 化学结构
CAS号：136790-76-6
Lubiprostone/鲁比前列素 3D分子结构
CAS号：136790-76-6
Lubiprostone/鲁比前列素 化学结构 CAS号：136790-76-6
Lubiprostone/鲁比前列素 3D分子结构 CAS号：136790-76-6
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Lubiprostone/鲁比前列素 纯度/质量文件 产品仅供科研

货号：A126294 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 CFTR ↓ 其他靶点 纯度
Ataluren ✔ 98%
Lumacaftor ++++

F508del-CFTR, EC50: 0.1 μM

 		98%
CFTR(inh)-172 +++

CFTR, Ki: 300 nM

 		99%+
GlyH-101 +

CFTR, Ki: 4.3 μM

 		99%+
IOWH-032 ++

CFTR, IC50: 1.01 μM

 		99%+
Tezacaftor ✔ 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Lubiprostone/鲁比前列素 生物活性

描述 As one of the nine members of the ClC family, ClC-2 (chloride channel type-2) is broadly expressed throughout the body, including the gastrointestinal tract [6]. Lubiprostone, a possible ClC-2 channel opener indicated for the treatment of constipation, increases chloride ion transport and fluid secretion into the intestinal lumen. Lubiprostone (3 nM–10 μM) induced a concentration-dependent contraction of the longitudinal muscle, with a pEC50 of 7.0 and maximal effect of 95±3% of the response to 1 μM PGE2 (n=4). Lubiprostone also caused a concentration-dependent contraction of circular muscle preparations. In rat colon longitudinal muscle, lubiprostone (10 nM–10 μM) caused a muscle contraction (maximum at 10 μM; 140±74% of the response to 1 μM PGE2, n=4). In human proximal stomach longitudinal muscle, lubiprostone induced a concentration-dependent contraction with a pEC50 of 6.4±0.2 and maximal effect at 10 μM of 102±17% of the response to 1 μM PGE2 (n=3) [7].

Lubiprostone/鲁比前列素 细胞实验

Cell Line
Concentration Treated Time Description References
T84 cells 0.001–10 μM 30 minutes To investigate the effect of Lubiprostone on the internalization and translocation of E. coli and S. typhimurium in T84 cell monolayers, results showed that Lubiprostone significantly reduced bacterial translocation in a concentration-dependent manner. Gut Microbes. 2012 May-Jun;3(3):250-60
T84 cells 100 nM 24 hours To evaluate the effect of Lubiprostone on Cl- secretion and fluid transport in T84 cells, results showed that Lubiprostone induced the highest Cl- secretion and fluid transport response among the secretagogues tested. Gut Microbes. 2012 May-Jun;3(3):250-60
Human conjunctival fibroblasts (HConFs) 10-300 nM 48 hours To investigate the effect of Lubiprostone on HConFs proliferation, results showed that Lubiprostone promoted cell proliferation in a dose-dependent manner, with peak effect at 100 nM. Int J Mol Med. 2018 Mar;41(3):1331-1338
HEK-293 cells 0.1 μM To test the effect of Lubiprostone on ClC-2 mediated currents, results showed no effect of Lubiprostone on ClC-2 currents Cells. 2020 Jul 26;9(8):1781

Lubiprostone/鲁比前列素 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Sheep Sheep tracheal epithelium Apical or basolateral 200 nM Investigate the effects of Lubiprostone on tracheal epithelium and submucosal gland secretion, identifying EP4 receptors as the target Br J Pharmacol. 2011 Jan;162(2):508-20
C57Bl/6 mice Oral gavage 1 mg/kg/day Once daily for 7 days To assess the effect of Lubiprostone on the colonic microbiome in mice, results showed that Lubiprostone significantly altered the composition of the intestinal microbiota, particularly within the Firmicutes and Bacteroidetes phyla. Gut Microbes. 2012 May-Jun;3(3):250-60
Rat Sprague-Dawley rats In vitro tissue bath 0.1 nM–10 µM Single administration Investigated the effects of Lubiprostone on rat stomach and colon muscle contractions, finding it induces contraction and inhibits neuronally mediated contractions via EP1 and EP4 receptor activation. Br J Pharmacol. 2008 May;154(1):126-35
Mice Acute constipation model (induced by scopolamine or loperamide) Oral 0.5 mg/kg Single dose To compare the efficacy of CFTR act-J027 with lubiprostone and linaclotide in increasing intestinal secretion and improving constipation models, results showed that CFTR act-J027 was more effective Transl Res. 2017 Apr;182:14-26. e4
Rats Chronic intermittent water avoidance stress (WAS) model Oral 10 μg/Kg Twice daily for 10 days Lubiprostone treatment significantly reduced WAS-induced changes in intestinal epithelial paracellular permeability and visceral hyperalgesia in a subpopulation of rats and prevented WAS-induced decrease in the epithelial tight junction protein Occludin (Ocln). Pain. 2018 Sep;159(9):1777-1789
Mice Clcn2−/− mice and Cftrtm1Eur mice Apical administration 0.1 μM To test the effect of Lubiprostone on secretory current in colonic epithelium, results showed Lubiprostone still elicited secretory current in ClC-2 deficient mice but not in CFTR deficient mice Cells. 2020 Jul 26;9(8):1781

Lubiprostone/鲁比前列素 动物研究

Dose Mice: 500 μg/kg/day[3] (p.o.)
Rat: 0.1 mg/kg - 1 mg/kg[4] (p.o.)
Administration p.o.
Pharmacokinetics
Animal Rats[5] Dogs[5]
Dose 50 μg/kg 5 μg/kg
Administration p.o. p.o.
AUC0→24h 63.4 ng eq·h/ml 14.5 ± 2.2 ng eq.·h/ml
AUC0→last 10.2 ng eq·h/ml 12.5 ± 1.9 ng eq.·h/ml
T1/2 2.55 h
t1/2α 1.12 ± 0.02 h
t1/2β 2.48 ± 0.13 h
Tmax 0.25 h 0.58 ± 0.14 h
Cmax 10.60 ng eq/ml 6.31 ± 0.49 ng eq./ml
AUC0→∞ 28.0 ng eq·h/ml 13.4 ± 1.9 ng eq.·h/ml

Lubiprostone/鲁比前列素 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00953017 - Completed - -
NCT03720613 - Not yet recruiting November 1, 2025 -
NCT00577499 - Terminated(Recruitment was sub... 展开 >>optimal) 收起 << - -

Lubiprostone/鲁比前列素 参考文献

[1]Bijvelds MJ, Bot AG, et al. Activation of intestinal Cl- secretion by lubiprostone requires the cystic fibrosis transmembrane conductance regulator. Gastroenterology. 2009 Sep;137(3):976-85.

[2]Bassil AK, Borman RA, et al. Activation of prostaglandin EP receptors by lubiprostone in rat and human stomach and colon. Br J Pharmacol. 2008 May;154(1):126-35.

[3]Mishima E, Fukuda S, et al. Alteration of the Intestinal Environment by Lubiprostone Is Associated with Amelioration of Adenine-Induced CKD. J Am Soc Nephrol. 2015 Aug;26(8):1787-94.

[4]Hayashi S, Kurata N, et al. Lubiprostone prevents nonsteroidal anti-inflammatory drug-induced small intestinal damage by suppressing the expression of inflammatory mediators via EP4 receptors. J Pharmacol Exp Ther. 2014 Jun;349(3):470-9.

[5]RU 0211

[6]Ao M, Venkatasubramanian J, Boonkaewwan C, Ganesan N, Syed A, Benya RV, Rao MC. Lubiprostone activates Cl- secretion via cAMP signaling and increases membrane CFTR in the human colon carcinoma cell line, T84. Dig Dis Sci. 2011 Feb;56(2):339-51. doi: 10.1007/s10620-010-1495-8. Epub 2010 Dec 8. PMID: 21140215.

[7]Bassil AK, Borman RA, Jarvie EM, McArthur-Wilson RJ, Thangiah R, Sung EZ, Lee K, Sanger GJ. Activation of prostaglandin EP receptors by lubiprostone in rat and human stomach and colon. Br J Pharmacol. 2008 May;154(1):126-35. doi: 10.1038/bjp.2008.84. Epub 2008 Mar 10. PMID: 18332851; PMCID: PMC2438971.

Lubiprostone/鲁比前列素 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.56mL

0.51mL

0.26mL

12.81mL

2.56mL

1.28mL

25.61mL

5.12mL

2.56mL

Lubiprostone/鲁比前列素 技术信息

CAS号136790-76-6
分子式C20H32F2O5
分子量 390.46
SMILES Code CCCCC(F)(F)C(CC[C@@H]1[C@H](C(C[C@H]1O)=O)CCCCCCC(O)=O)=O
MDL No. MFCD20268389
别名 鲁比前列酮 ;SPI-0211; RU-0211
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, store in freezer, under -20°C
溶解方案

DMSO: 105 mg/mL(268.91 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三

Tags: Lubiprostone | 136790-76-6 | RU-0211 | SPI-0211 | RU0211 | RU 0211 | SPI0211 | SPI 0211 | SPI-0211 | Chloride Channel Activator | Membrane Transporter/Ion Channel | Chloride Channel | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Lubiprostone/鲁比前列素 纯度/质量文件 | Lubiprostone/鲁比前列素 亚型比较 | Lubiprostone/鲁比前列素 生物活性 | Lubiprostone/鲁比前列素 动物研究 | Lubiprostone/鲁比前列素 临床数据 | Lubiprostone/鲁比前列素 参考文献 | Lubiprostone/鲁比前列素 实验方案 | Lubiprostone/鲁比前列素 技术信息

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