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Postion:Product Catalog >Biochemical Engineering>Inhibitors>Transmembrane Transporters>CFTR activator>Lubiprostone
Lubiprostone
  • Lubiprostone

Lubiprostone NEW

Price $47 $77 $138
Package 5mg 10mg 25mg
Supply Ability: 10g
Update Time: 2026-06-02

Product Details

Product Name: Lubiprostone CAS No.: 136790-76-6
Purity: 98.83% Supply Ability: 10g
Release date: 2026/06/02

Product Introduction

Bioactivity

NameLubiprostone
DescriptionLubiprostone (RU-0211), an activator of ClC-2 chloride channels, is used in the therapy of idiopathic chronic constipation.
Kinase AssayFluorescence polarization-based competition assay: Inhibition constants ( Ki ) for the antagonists are determined by addition of the IAP protein constructs to wells containing serial dilutions of the antagonists or the peptide AVPW, and the Hid-FAM probe or AVP-diPhe-FAM probe, as appropriate, in the polarization buffer. Samples are read after a 30-minute incubation. Fluorescence polarization values are plotted as a function of the antagonist concentration, and the IC50 values are obtained by fitting the data to a 4-parameter equation using software. Ki values for the antagonists are determined from the IC50 valued.
In vitroLubiprostone 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 vivoLubiprostone induces a CdCl(2)-insensitive secretory response in mouse intestine, but fail to induce intestinal Cl(-) secretion in Cftr-null mice. [1]
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
Solubility InformationEthanol : 72 mg/mL (184.4 mM), Sonication is recommended.
DMSO : 245 mg/mL (627.47 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2.5 mg/mL (6.4 mM), Sonication is recommended.
10% DMSO+90% Saline : 10 mg/mL (25.61 mM), Suspension.
H2O : < 1 mg/mL (insoluble or slightly soluble)
KeywordsSPI0211 | SPI 0211 | RU0211 | RU 0211 | Lubiprostone | Inhibitor | inhibit | Cl? Channels | Chloridechannel | Chloride channel
Inhibitors RelatedKaolin | Ethyl palmitate | Gum arabic | Urethane | 1,8-Cineole | Aminopicoline | 1,4-Naphthoquinone | Tributyrin | Glucosamine | Methylene Blue trihydrate | Gluconate Calcium | Magnesium sulfate
Related Compound LibrariesBioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | FDA-Approved Drug Library | Anti-Cancer Approved Drug Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Ion Channel Targeted Library | Anti-COVID-19 Compound Library | Anti-Cancer Drug Library

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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TargetMol Chemicals Inc.

6YR United StatesUnited States
  • Since: 2011-01-07
  • Address: 36 Washington Street, Wellesley Hill, MA
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