Fulacimstat

This product is for research use only, not for human use. We do not sell to patients.

Fulacimstat
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Size Price Stock
100mg$1950Check With Us
250mg$3250Check With Us
500mg$4875Check With Us

Cat #: V4220 CAS #: 1488354-15-9 Purity ≥ 98%

Description: Fulacimstat (also known as BAY1142524) is a novel, potent and orally bioavailable chymase inhibitor with IC50s of 4, 3 nM for human and hamster chymase enzyme, respectively.

References: Hanna Tinel, et al. Abstract 13624: A Novel Chymase Inhibitor BAY 1142524 Reduces Fibrosis and Improves Cardiac Function After Myocardial Infarction in Hamster. Circulation. 2018;136:A13624.

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Molecular Weight (MW)487.39
Molecular FormulaC23H16F3N3O6
CAS No.1488354-15-9
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
SMILES CodeO=C(C1=CN(C2=CC=C3N(C)C(OC3=C2)=O)C(N([C@@H]4CCC5=C4C=CC=C5C(F)(F)F)C1=O)=O)
SynonymsFulacimstat; BAY-1142524; BAY 1142524; BAY1142524;
ProtocolIn VitroFulacimstat inhibits human and hamster chymase enzyme with IC50s of 4 nM and 3 nM, respectively.
In VivoIsoprenaline induces cardiac fibrosis (24.4±1.8%) in hamsters, which is reduced dose dependently by Fulacimstat (16.4±1.2%, 12.4 ± 1.3%, 10.9±1.4% at 1, 3 and 10 mg/kg respectively) and by enalapril (17.7±1.5% at 20 mg/kg). Four weeks after MI, hamster hearts show an increased end diastolic pressure, and reduce contractility and relaxation. Compared to placebo (19.3±2 mmHg), Fulacimstat at 10 mg/kg reduce significantly the end diastolic pressure (13.2±1.4 mmHg) without any effects on blood pressure or heart rate. Moreover, treatment with Fulacimstat reduce the fibrotic area and improve the cardiac response to adrenergic stimulation.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.0517 mL10.2587 mL20.5175 mL41.0349 mL
5mM0.4103 mL2.0517 mL4.1035 mL8.2070 mL
10mM0.2052 mL1.0259 mL2.0517 mL4.1035 mL
20mM0.1026 mL0.5129 mL1.0259 mL2.0517 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

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 add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.