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Fulacimstat Serine Protease inhibitor

Name: Fulacimstat
Brand: Selleck Chemicals
SKU: S0042
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S0042

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

Chemical Structure

Molecular Weight: 487.38

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
HPLC
SDS
Datasheet

99.45

Related Targets	HDAC Caspase Proteasome Secretase MMP HCV Protease Cysteine Protease DPP Tyrosinase HIV Protease
Other Serine Protease Inhibitors	Leupeptin Hemisulfate PMSF Nafamostat mesilate (FUT-175) Sivelestat AEBSF HCl Gabexate Mesylate Alvelestat (AZD9668) Sivelestat sodium tetrahydrate UK-371804 HCl Ulinastatin

Solubility

In vitro
Batch:

DMSO : 97 mg/mL (199.02 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection 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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.850mg/ml (9.95mM)	Taking the 1 mL working solution as an example, add 50 μL of 97 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.800mg/ml (1.64mM)	Taking the 1 mL working solution as an example, add 50 μL of 16 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

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.

Chemical Information, Storage & Stability

Molecular Weight	487.38	Formula	C₂₃H₁₆F₃N₃O₆	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1488354-15-9	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	BAY1142524			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

Mechanism of Action

Targets/IC₅₀/Ki	hamster chymase enzyme (Cell-free assay) 3 nM human chymase enzyme (Cell-free assay) 4 nM
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.
References	[1] https://www.ahajournals.org/doi/abs/10.1161/circ.136.suppl_1.13624

Clinical Trial Information

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

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03402438	Completed	Clinical Trial Phase I	Bayer	February 12 2018	Phase 1

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