Home Transmembrane Transporters Chloride Channel activator Lubiprostone For research use only.

Lubiprostone

Synonyms: RU 0211,SPI-0211

Lubiprostone (RU 0211,SPI-0211) is an activator of ClC-2 chloride channels, used in the management of idiopathic chronic constipation.

Lubiprostone Chemical Structure

Lubiprostone Chemical Structure

CAS: 136790-76-6

Purity & Quality Control

Batch: Purity: 100.0%
100.0

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Biological Activity

Description Lubiprostone (RU 0211,SPI-0211) is an activator of ClC-2 chloride channels, used in the management of idiopathic chronic constipation.
Targets
ClC-2 chloride channels [1]
In vitro
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]
In Vivo
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01469819 Completed Chronic Idiopathic Constipation Texas Tech University Health Sciences Center El Paso|Takeda Pharmaceuticals North America Inc. June 2012 Phase 2|Phase 3
NCT01324284 Completed Colorectal Carcinoma Asian Institute of Gastroenterology India March 2011 Phase 3
NCT00934479 Completed Other Constipation|Irritable Bowel Syndrome Mayo Clinic|Arizona State University|Takeda Pharmaceuticals North America Inc. April 2010 Phase 1
NCT01085643 Completed 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 --

Chemical lnformation & Solubility

Molecular Weight 390.46 Formula

C20H32F2O5
CAS No. 136790-76-6 SDF Download Lubiprostone SDF
Smiles CCCCC(C1(CCC2C(O1)CC(=O)C2CCCCCCC(=O)O)O)(F)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 78 mg/mL ( (199.76 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 78 mg/mL

Water : Insoluble


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In vivo
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