Home Neuronal Signaling AChR antagonist Revefenacin For research use only.

Revefenacin

Synonyms: TD-4208, GSK-1160724

Revefenacin (TD-4208, GSK-1160724) is a potent, lung-selective, long-acting muscarinic antagonist that may be for the treatment of respiratory disease.

Revefenacin Chemical Structure

Revefenacin Chemical Structure

CAS: 864750-70-9

Purity & Quality Control

Batch: S525801 DMSO] 100 mg/mL] false] Ethanol] 100 mg/mL] false] Water] Insoluble] false Purity: 99.94%
99.94

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Signaling Pathway

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AChR Signaling Pathway

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Biological Activity

Description Revefenacin (TD-4208, GSK-1160724) is a potent, lung-selective, long-acting muscarinic antagonist that may be for the treatment of respiratory disease.
Targets
mAChR [1]
In vitro
In vitro Revefenacin is a high affinity competitive antagonist at human recombinant mAChRs with kinetic functional selectivity for M3 over M2 mAChRs and a potent, slowly reversible antagonist in rat, guinea pig, and human airway tissues expressing native mAChRs[1].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02772159 Completed
Chronic Obstructive Pulmonary Disease (COPD)
Mylan Inc.|Theravance Biopharma|Viatris Inc.
 June 2015 Phase 1
NCT00555022 Completed
Pulmonary Disease Chronic Obstructive
GlaxoSmithKline
 December 12 2007 Phase 1

Chemical Information & Solubility

Molecular Weight 597.75 Formula

C35H43N5O4
CAS No. 864750-70-9 SDF --
Smiles CN(CCN1CCC(CC1)OC(=O)NC2=CC=CC=C2C3=CC=CC=C3)C(=O)C4=CC=C(C=C4)CN5CCC(CC5)C(=O)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (167.29 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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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.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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