Fulacimstat

Catalog No.S0042 Synonyms: BAY1142524

For research use only.

Fulacimstat (BAY1142524) is an orally available inhibitor of chymase with IC50 of 4 nM and 3 nM for human and hamster chymase enzyme, respectively.

Fulacimstat Chemical Structure

CAS No. 1488354-15-9

Purity & Quality Control

Choose Selective Serine Protease Inhibitors

Biological Activity

Description Fulacimstat (BAY1142524) is an orally available inhibitor of chymase with IC50 of 4 nM and 3 nM for human and hamster chymase enzyme, respectively.
Targets
hamster chymase enzyme [1]
(Cell-free assay)
human chymase enzyme [1]
(Cell-free assay)
3 nM 4 nM

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 97 mg/mL
(199.02 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 487.38
Formula

C23H16F3N3O6

CAS No. 1488354-15-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1C2=C(C=C(C=C2)N3C=C(C(=O)N(C3=O)C4CCC5=C4C=CC=C5C(F)(F)F)C(=O)O)OC1=O

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

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% DMSO % % Tween 80 % ddH2O
%DMSO %

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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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03402438 Completed Drug: Fulacimstat (BAY1142524) Clinical Trial Phase I Bayer February 12 2018 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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