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Lubiprostone Chloride Channel activator

Name: Lubiprostone
SKU: S1675
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S1675

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

Chemical Structure

Molecular Weight: 390.46

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.93%

99.93

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Chemical Information, Storage & Stability

Molecular Weight	390.46	Formula	C₂₀H₃₂F₂O₅	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	136790-76-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	RU 0211,SPI-0211			Smiles	CCCCC(C1(CCC2C(O1)CC(=O)C2CCCCCCC(=O)O)O)(F)F

Solubility

In vitro
Batch:

DMSO : 79 mg/mL (202.32 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 79 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 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.

Mechanism of Action

Targets/IC₅₀/Ki	ClC-2 chloride channels ^[1]
In vitro	Lubiprostone induces a robust secretory response in T84 monolayers. This compound induces a rise in cAMP levels that was sensitive to EP(4)-receptor blockage in T84 cells. ^[1] It also 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. This chemical also reduces electrically stimulated, neuronal contractions in rat and human colon circular muscle preparations. ^[2] It (1 mM) stimulates higher elevations in TER despite lower I(sc) responses compared with the nonselective secretory agonist PGE(2) (1 mM). The compound 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] It causes comparable and maximal increases of I(sc) in T84 cells. Lubiprostone-induced increases in iodide efflux are ~80% of those obtained with forskolin. This agent activates Cl(-) secretion in T84 cells via cAMP, protein kinase A, and by increasing apical membrane CFTR protein. ^[4] When applied to the small intestinal mucosa in eight concentrations ranging from 1-3000 nM, it evokes increases in Isc in a concentration-dependent manner with an EC50 of 42.5 nM. Applied to the mucosa of the colon in eight concentrations ranging from 1-3000 nM, this compound evokes increases in Isc in a concentration-dependent manner with an EC50 of 31.7 nM. ^[5]
In vivo	Lubiprostone induces a CdCl(2)-insensitive secretory response in mouse intestine, but this compound fails to induce intestinal Cl(-) secretion in Cftr-null mice. ^[1]
References	[1] https://pubmed.ncbi.nlm.nih.gov/19454284/ [2] https://pubmed.ncbi.nlm.nih.gov/18332851/ [3] https://pubmed.ncbi.nlm.nih.gov/17053162/ [4] https://pubmed.ncbi.nlm.nih.gov/21140215/ [5] https://pubmed.ncbi.nlm.nih.gov/19179625/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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	--

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