Home Proteases Serine Protease inhibitor Fulacimstat For research use only.

Fulacimstat

Synonyms: BAY1142524

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

Fulacimstat Chemical Structure

CAS No. 1488354-15-9

Purity & Quality Control

Batch: S004201 DMSO]97 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.45%
99.45

Fulacimstat Related Products

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
In Vivo
In vivo

The chymase inhibitor Fulacimstat (BAY1142524) reduces cardiac fibrosis in hamster, attenuating the deterioration of heart function after myocardial infarction and preserving the contractile reserve of the heart.[1]
Animal Research Animal Models Male Syrian hamsters
Dosages 10 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03402438 Completed
Clinical Trial Phase I
Bayer
 February 12 2018 Phase 1

Chemical Information & Solubility

Molecular Weight 487.38 Formula

C23H16F3N3O6
CAS No. 1488354-15-9 SDF --
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
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 97 mg/mL ( (199.02 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)

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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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