Lubiprostone | 鲁比前列酮 | SPI-0211 | Chloride Channel Activator

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

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

Lubiprostone is an ClC-2 chloride channel activator used in the treatment of idiopathic chronic constipation.

Lubiprostone 化学结构
CAS号：136790-76-6

Lubiprostone 3D分子结构
CAS号：136790-76-6

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Lubiprostone 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]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nat. Biomed. Eng., 2024, 8, 1412-1424. Ambeed. [ A538667 , A631746 ]; • JMC, 2024. Ambeed. [ A833302 , A475501 , A341986 , A356070 ]; • BMC Cancer, 2024, 24(1): 1415. Ambeed. [ A809692 , A209020 ]; • J. Am. Soc. Mass Spectrom., 2024, 35(12): 3192-3202. Ambeed. [ A166127 , A902473 , A753371 , A961334 , A292945 , A230770 , A300620 , A1114580 , A1159765 , A206238 ]; • PloS One, 2024, 19(11): e0308060. Ambeed. [ A302917 ]; 更多 >

CFTR 亚型比较

产品名称	CFTR ↓ ↑	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 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 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.
AUC_0→24h	63.4 ng eq·h/ml	14.5 ± 2.2 ng eq.·h/ml
AUC_0→last	10.2 ng eq·h/ml	12.5 ± 1.9 ng eq.·h/ml
T_1/2	2.55 h
t_1/2α		1.12 ± 0.02 h
t_1/2β		2.48 ± 0.13 h
T_max	0.25 h	0.58 ± 0.14 h
C_max	10.60 ng eq/ml	6.31 ± 0.49 ng eq./ml
AUC_0→∞	28.0 ng eq·h/ml	13.4 ± 1.9 ng eq.·h/ml

Lubiprostone 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 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 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 技术信息

CAS号	136790-76-6
分子式	C₂₀H₃₂F₂O₅
分子量	390.462

别名	鲁比前列酮 ;SPI-0211;RU-0211
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

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

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

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 <<	-	-
NCT02481947	Chronic Idiopathic Constipatio... 展开 >>n 收起 <<	Phase 3	Completed	-	-
NCT00399542	Irritable Bowel Syndrome ... 展开 >> Constipation 收起 <<	Phase 3	Completed	-	-
NCT01298219	Opioid-induced Bowel Dysfuncti... 展开 >>on 收起 <<	Phase 3	Completed	-	-
NCT00399542	-		Completed	-	-
NCT00380250	Irritable Bowel Syndrome With ... 展开 >>Constipation 收起 <<	Phase 3	Completed	-	-
NCT00611442	Bowel Preparation for Colonosc... 展开 >>opy 收起 <<	Not Applicable	Completed	-	United States, Texas ... 展开 >> Brooke Army Medical Center Fort Sam Houston, Texas, United States, 78234 收起 <<
NCT00611442	-		Completed	-	-
NCT01372423	Chronic Idiopathic Constipatio... 展开 >>n 收起 <<	Phase 3	Completed	-	-
NCT01162863	Irritable Bowel Syndrome ... 展开 >> Constipation 收起 <<	Not Applicable	Completed	-	United States, Michigan ... 展开 >> University of Michigan Health System Ann Arbor, Michigan, United States, 48103 收起 <<
NCT00985569	-		Withdrawn(Enrollment was never... 展开 >> begun.) 收起 <<	November 2010	United States, Florida ... 展开 >> Geriatric Medical Associates Brooksville, Florida, United States Cassellberry Family Practice Casselberry, Florida, United States Osler Geriatrics Melbourne, Florida, United States 收起 <<
NCT00953017	Colonoscopy	Phase 4	Completed	-	United States, Texas ... 展开 >> Brooke Army Medical Center San Antonio, Texas, United States, 78248 收起 <<
NCT01993875	Chronic Idiopathic Constipatio... 展开 >>n 收起 <<	Phase 3	Completed	-	United States, Alabama ... 展开 >> Anniston, Alabama, United States, 36207 United States, California Anaheim, California, United States, 92801 United States, Florida Deland, Florida, United States, 32720 Hollywood, Florida, United States, 33024 Orlando, Florida, United States, 32809 South Miami, Florida, United States, 33143 United States, Kansas Overland Park, Kansas, United States, 66212 United States, New Jersey Marlton, New Jersey, United States, 08053 United States, North Carolina Raleigh, North Carolina, United States, 27612 United States, Utah Salt Lake City, Utah, United States, 84106 United States, Wisconsin West Bend, Wisconsin, United States, 53095 收起 <<
NCT01674530	Chronic Idiopathic Constipatio... 展开 >>n 收起 <<	Phase 3	Completed	-	-
NCT00934479	Other Constipation ... 展开 >> Irritable Bowel Syndrome 收起 <<	Phase 1	Completed	-	United States, Arizona ... 展开 >> Mayo Clinic Arizona Scottsdale, Arizona, United States, 85259 收起 <<
NCT00452335	Constipation	Phase 4	Completed	-	United States, Arizona ... 展开 >> Phoenix Children's Hospital Pheonix, Arizona, United States, 85016 United States, Arkansas Arkansas Pediatric Clinic Little Rock, Arkansas, United States, 72005 United States, California Children's Hospital and Research Center Oakland Oakland, California, United States, 94609 United States, Florida Nemours Children's Clinic - Jacksonville Jacksonville, Florida, United States, 32207 Nemours Children's Clinic - Pensacola Pensacola, Florida, United States, 32504 United States, Illinois Center for Children's Digestive Health Park Ridge, Illinois, United States, 60068 University of Illinois at Peoria Peoria, Illinois, United States, 61613 University of Illinois at Chicago Springfield, Illinois, United States, 62708-0787 United States, Indiana Indiana University Indianapolis, Indiana, United States, 46202 United States, Kansas University of Kansas Medical Center Kansas City, Kansas, United States, 66160 United States, Massachusetts Children's Hospital Boston Boston, Massachusetts, United States, 02115 United States, Nebraska The Center for Human Nutrition, Inc. Omaha, Nebraska, United States, 68105 United States, New Jersey AHS Hospital Corporation Morristown, New Jersey, United States, 07962 United States, Ohio Children's Research Institute Columbus, Ohio, United States, 43205 Pediatric Associates of Fairfield, Inc. Fairfield, Ohio, United States, 45014 United States, Pennsylvania Regional Gastroenterology Associates of Lancaster, Ltd. Lancaster, Pennsylvania, United States, 17604 United States, Tennessee Southeastern Clinical Research Chattanooga, Tennessee, United States, 37403 Jackson Clinic Jackson, Tennessee, United States, 38305 United States, Wisconsin Medical College of Wisconsin Milwaukee, Wisconsin, United States, 53226 收起 <<
NCT00452335	-		Completed	-	-
NCT00595946	Opioid-Induced Bowel Dysfuncti... 展开 >>on 收起 <<	Phase 3	Completed	-	-
NCT00595946	-		Completed	-	-
NCT00597428	Opioid-Induced Bowel Dysfuncti... 展开 >>on 收起 <<	Phase 3	Completed	-	-
NCT01460225	Chronic Idiopathic Constipatio... 展开 >>n 收起 <<	Phase 4	Completed	-	United States, New Hampshire ... 展开 >> Dartmouth-Hitchcock Medical Center Lebanon, New Hampshire, United States, 03756 收起 <<
NCT00380250	-		Completed	-	-
NCT01162863	-		Completed	-	-
NCT01460225	-		Completed	-	-
NCT00620061	Opioid-Induced Bowel Dysfuncti... 展开 >>on 收起 <<	Phase 3	Completed	-	-
NCT00689026	Diabetes Mellitus, Type 1 ... 展开 >> Diabetes Mellitus, Type 2 收起 <<	Not Applicable	Terminated	-	United States, Georgia ... 展开 >> Medical College of Georgia Augusta, Georgia, United States, 30912 收起 <<
NCT00662363	Constipation	Not Applicable	Completed	-	United States, Illinois ... 展开 >> Rehabilitation Institute of Chicago Chicago, Illinois, United States, 60302 收起 <<
NCT00597428	-		Completed	-	-
NCT00662363	-		Completed	-	-
NCT00746395	-		Completed	-	-
NCT00746395	Inflammatory Bowel Disease	Phase 4	Completed	-	United States, Alabama ... 展开 >> USA Pavilion at Infirmary West Mobile, Alabama, United States, 36693 收起 <<
NCT00844831	Constipation	Phase 4	Completed	-	United States, Kentucky ... 展开 >> University of Louisville Louisville, Kentucky, United States, 40202 收起 <<
NCT00689026	-		Terminated	-	-
NCT02042183	Constipation - Functional	Phase 3	Completed	-	-
NCT01096290	Constipation	Phase 4	Completed	-	United States, Alabama ... 展开 >> USA Pavilion at Infirmary West Mobile, Alabama, United States, 36693 收起 <<
NCT00669461	-		Terminated(Lack of recruitment... 展开 >>) 收起 <<	-	-
NCT00706004	Constipation ... 展开 >>Cystic Fibrosis 收起 <<	Not Applicable	Completed	-	United States, Arkansas ... 展开 >> University of Arkansas for Medical Sciences Little Rock, Arkansas, United States, 72205 收起 <<
NCT00706004	-		Completed	-	-
NCT02544152	Irritable Bowel Syndrome	Phase 2	Terminated	-	United States, Alabama ... 展开 >> E Squared Research, Inc. Huntsville, Alabama, United States, 35801 United States, Arkansas Arkansas Gastroenterology North Little Rock, Arkansas, United States, 72117 United States, California GW Research Inc. Chula Vista, California, United States, 91910 Inland Empire Liver Foundation Rialto, California, United States, 92377 United States, Florida Prestige Clinical Research Center Miami, Florida, United States, 33133 Advanced Gastroenterology Associates, LLC Palm Harbor, Florida, United States, 34684 United States, Maryland Meritus Center for Clinical Research Hagerstown, Maryland, United States, 21742 United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 United States, North Carolina PMG Research of Charlotte Charlotte, North Carolina, United States, 28210 PMG Research of Charlotte Concord, North Carolina, United States, 28025 Cumberland Research Associates, LLC Fayetteville, North Carolina, United States, 28304 Wake Research Associates, LLC Raleigh, North Carolina, United States, 27612 United States, Tennessee Clinical Research Solutions Jackson, Tennessee, United States, 38305 United States, Texas Houston Endoscopy Research Center Houston, Texas, United States, 77079 Wellness Clinical Research Associates McKinney, Texas, United States, 75071 Advanced Clinical Research Associates Plano, Texas, United States, 75093 收起 <<
NCT00844831	-		Completed	-	-
NCT01166789	Irritable Bowel Syndrome	Phase 1	Completed	-	United States, North Carolina ... 展开 >> UNC Clinical and Translational Research Center Chapel Hill, North Carolina, United States, 27599 收起 <<
NCT00953043	-		Completed	-	-
NCT00908076	Parkinson's Disease	Phase 4	Completed	-	United States, Florida ... 展开 >> University of South Florida Tampa, Florida, United States, 33606 United States, Texas Baylor College of Medicine PDCMDC Houston, Texas, United States, 77030 收起 <<
NCT00908076	-		Completed	-	-
NCT00645801	Colonoscopy	Phase 4	Completed	-	United States, Michigan ... 展开 >> Henry Ford Hospital Detroit, Michigan, United States, 48202 Henry Ford Health System Novi, Michigan, United States, 48377 收起 <<
NCT00953043	Healthy	Phase 4	Completed	-	United States, Minnesota ... 展开 >> Mayo Clinic Rochester, Minnesota, United States, 55905 收起 <<
NCT01170039	Constipation ... 展开 >>Diabetes 收起 <<	Phase 4	Completed	-	United States, Georgia ... 展开 >> Atlanta Veterans Administration Hospital Atlanta, Georgia, United States, 30033 The Emory Clinic Atlanta, Georgia, United States, 30322 收起 <<
NCT00669461	Constipation ... 展开 >>Parkinson's Disease 收起 <<	Not Applicable	Terminated(Lack of recruitment... 展开 >>) 收起 <<	-	United States, Arkansas ... 展开 >> University of Arkansas for Medical Sciences Little Rock, Arkansas, United States, 72205 收起 <<
NCT01236534	-		Completed	-	-
NCT01839734	HIV	Phase 2	Unknown	June 2015	United States, Illinois ... 展开 >> Ruth M. Rothstein CORE Center Chicago, Illinois, United States, 60612 收起 <<
NCT01190020	Chronic Constipation, Methanog... 展开 >>enesis 收起 <<	Phase 1	Unknown	-	United States, Iowa ... 展开 >> University of Iowa Hospitals and Clinics Recruiting Iowa City, Iowa, United States, 52242 收起 <<
NCT01170039	-		Completed	-	-
NCT03010631	Healthy Volunteers	Phase 3	Completed	-	United States, Texas ... 展开 >> ICON San Antonio, Texas, United States, 78209 收起 <<
NCT01447849	Constipation	Phase 2 Phase 3	Completed	-	United States, Texas ... 展开 >> Texas Tech University Health Sciences Center El Paso, Texas, United States, 79905 收起 <<
NCT01085643	Constipation-predominant Irrit... 展开 >>able Bowel Syndrome 收起 <<	Not Applicable	Completed	-	United States, California ... 展开 >> Cedars-Sinai Medical Center Los Angeles, California, United States, 90048 收起 <<
NCT01085643	-		Completed	-	-
NCT02138136	Constipation - Functional	Phase 3	Completed	-	-
NCT01447849	-		Completed	-	-
NCT02651155	-		Completed	-	-
NCT01469819	Chronic Idiopathic Constipatio... 展开 >>n 收起 <<	Phase 2 Phase 3	Completed	-	United States, Texas ... 展开 >> Texas Tech University Health Sciences Center El Paso, Texas, United States, 79905 收起 <<
NCT01236534	Multiple Sclerosis ... 展开 >> Constipation 收起 <<	Phase 4	Completed	-	United States, New York ... 展开 >> University of Rochester Rochester, New York, United States, 14642 收起 <<
NCT01469819	-		Completed	-	-
NCT01324284	Colorectal Carcinoma	Phase 3	Completed	-	-
NCT03097861	Chronic Idiopathic Constipatio... 展开 >>n 收起 <<	Phase 3	Completed	-	-
NCT02695719	Constipation	Phase 3	Completed	-	Korea, Republic of ... 展开 >> Cheonan-si, Chungcheongnam-do, Korea, Republic of Seongnam-si, Gyeonggi-do, Korea, Republic of Iksan-si, Jeollabuk-do, Korea, Republic of Daejeon, Korea, Republic of Seoul, Korea, Republic of 收起 <<
NCT02651155	Constipation	Phase 3	Completed	-	Russian Federation ... 展开 >> Saint-Petersburg, Pushkin, Russian Federation Barnaul, Russian Federation Kazan, Russian Federation Kemerovo, Russian Federation Krasnodar, Russian Federation Moscow, Russian Federation Novosibirsk, Russian Federation Omsk, Russian Federation Saint Petersburg, Russian Federation Saint-Petersburg, Russian Federation Samara, Russian Federation Ulyanovsk, Russian Federation Yaroslavl, Russian Federation 收起 <<
NCT02729909	Constipation	Phase 3	Completed	-	Mexico ... 展开 >> Mexicali, Baja California Norte, Mexico Mexico, Distrito Federal, Mexico Cuautitlan Izcalli, Estado de Mexico, Mexico Tlalnepantla, Estado de Mexico, Mexico Leon, Guanajuato, Mexico Morelia, Michoacan, Mexico Monterrey, Nuevo Le0n, Mexico Culiacan, Sinaloa, Mexico Chihuahua, Mexico Durango, Mexico 收起 <<
NCT02766777	Constipation - Functional	Phase 3	Completed	-	United States, Arkansas ... 展开 >> Northwest Arkansas Pediatric Clinic Fayetteville, Arkansas, United States, 72703 United States, Illinois Methodist Medical Center Peoria, Illinois, United States, 61602 United States, Louisiana Willis-Knighton Physician Network Shreveport, Louisiana, United States, 71101 United States, Nebraska Pioneer Clinical Research Bellevue, Nebraska, United States, 68005 United States, Ohio PriMed Clinical Research Beavercreek, Ohio, United States, 45431 United States, Oregon Cyn3rgy Research Gresham, Oregon, United States, 97030 United States, South Carolina Coastal Clinical Research Charleston, South Carolina, United States, 29414 Coastal Pediatrics Associates - Mount Pleasant Mount Pleasant, South Carolina, United States, 29464 Spartanburg Medical Research Spartanburg, South Carolina, United States, 29303 United States, Texas 3rd Coast Research Associates Corpus Christi, Texas, United States, 78413 United States, Utah Bridgerland Clinical Research Logan, Utah, United States, 84341 Wee Care Pediatrics Syracuse, Utah, United States, 84075 United States, Virginia Pediatric Research of Charlottesville, LLC Charlottesville, Virginia, United States, 22902 收起 <<

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

Lubiprostone 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Lubiprostone 质控信息

Lubiprostone 生物活性

Lubiprostone 动物研究

Lubiprostone 临床研究

Lubiprostone 参考文献

Lubiprostone 实验方案

Lubiprostone 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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

Lubiprostone 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Lubiprostone 质控信息

Lubiprostone 生物活性

Lubiprostone 动物研究

Lubiprostone 临床研究

Lubiprostone 参考文献

Lubiprostone 实验方案

Lubiprostone 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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Lubiprostone 纯度/质量文件产品仅供科研