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Lubiprostone

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Chemical Structure| 136790-76-6 同义名 : 鲁比前列酮 ;SPI-0211;RU-0211
CAS号 : 136790-76-6
货号 : A126294
分子式 : C20H32F2O5
纯度 : 99%+
分子量 : 390.462
MDL号 : MFCD20268389
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

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
动物实验配方：
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].
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 << - -
实验方案
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
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.