Lubiprostone
For research use only.
Catalog No.S1675 Synonyms: RU 0211

CAS No. 136790-76-6
Lubiprostone (RU 0211) is an activator of ClC-2 chloride channels, used in the management of idiopathic chronic constipation.
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Biological Activity
Description | Lubiprostone (RU 0211) is an activator of ClC-2 chloride channels, used in the management of idiopathic chronic constipation. | |
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Targets |
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In vitro |
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] |
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In vivo | Lubiprostone induces a CdCl(2)-insensitive secretory response in mouse intestine, but fail to induce intestinal Cl(-) secretion in Cftr-null mice. [1] |
Protocol
Solubility (25°C)
In vitro | DMSO | 78 mg/mL (199.76 mM) |
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Ethanol | 78 mg/mL (199.76 mM) | |
Water | Insoluble |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
Molecular Weight | 390.46 |
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Formula | C20H32F2O5 |
CAS No. | 136790-76-6 |
Storage |
powder in solvent |
Synonyms | RU 0211 |
Smiles | CCCCC(C1(CCC2C(O1)CC(=O)C2CCCCCCC(=O)O)O)(F)F |
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment) | ||||||||||
Dosage | mg/kg | Average weight of animals | g | Dosing volume per animal | ul | Number of animals | ||||
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% DMSO % % Tween 80 % ddH2O | ||||||||||
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: : mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL,)
Method for preparing in vivo formulation:Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80,mix and clarify, next add μL ddH2O,mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Clinical Trial Information
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
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NCT01469819 | Completed | Drug: Lubiprostone | Chronic Idiopathic Constipation | Texas Tech University Health Sciences Center El Paso|Takeda Pharmaceuticals North America Inc. | June 2012 | Phase 2|Phase 3 |
NCT01324284 | Completed | Drug: Lubiprostone | Colorectal Carcinoma | Asian Institute of Gastroenterology India | March 2011 | Phase 3 |
NCT00934479 | Completed | Drug: Lubiprostone | Other Constipation|Irritable Bowel Syndrome | Mayo Clinic|Arizona State University|Takeda Pharmaceuticals North America Inc. | April 2010 | Phase 1 |
NCT01085643 | Completed | Drug: Lubiprostone|Drug: Placebo | Constipation-predominant Irritable Bowel Syndrome | Cedars-Sinai Medical Center|Takeda Pharmaceuticals North America Inc. | March 2010 | Not Applicable |
NCT00985569 | Withdrawn | -- | Constipation | Synergy Health Solutions | November 2009 | -- |
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