Lotamilast (RVT-501)

Synonyms: E6005

Lotamilast (RVT-501, E6005) is a selective phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 2.8 nM.

Lotamilast (RVT-501) Chemical Structure

Lotamilast (RVT-501) Chemical Structure

CAS: 947620-48-6

Purity & Quality Control

Batch: S019001 DMSO] 94 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.66%
99.66

Lotamilast (RVT-501) Related Products

Signaling Pathway

Choose Selective PDE Inhibitors

Biological Activity

Description Lotamilast (RVT-501, E6005) is a selective phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 2.8 nM.
Targets
PDE4 [1]
(in phosphodiesterase assay)
2.8 nM
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03415282 Unknown status
Atopic Dermatitis
Dermavant Sciences GmbH|Dermavant Sciences Inc.
February 5 2018 Phase 1
NCT03394677 Completed
Atopic Dermatitis
Dermavant Sciences GmbH|Dermavant Sciences Inc.
January 25 2018 Phase 2
NCT02094235 Completed
Atopic Dermatitis
Dermavant Sciences GmbH|Dermavant Sciences Inc.
January 2014 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 472.49 Formula

C26H24N4O5

CAS No. 947620-48-6 SDF --
Smiles CNC1=NC2=CC(=C(C=C2C(=N1)C3=CC(=CC=C3)NC(=O)C4=CC=C(C=C4)C(=O)OC)OC)OC
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 94 mg/mL ( (198.94 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : 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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Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

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.

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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