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Fulacimstat (Synonyms: BAY1142524)

Cat. No.: HY-109059
Handling Instructions

Fulacimstat is an orally available chymase inhibitor, with IC50s of 4, 3 nM for human and hamster chymase enzyme, respectively.

For research use only. We do not sell to patients.

Fulacimstat Chemical Structure

Fulacimstat Chemical Structure

CAS No. : 1488354-15-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 500 In-stock
Estimated Time of Arrival: December 31
25 mg USD 950 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2450 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

Fulacimstat is an orally available chymase inhibitor, with IC50s of 4, 3 nM for human and hamster chymase enzyme, respectively.

IC50 & Target

IC50: 4 nM (human chymase enzyme), 3 nM (hamster chymase enzyme)[1][2].

In Vitro

Fulacimstat inhibits human and hamster chymase enzyme with IC50s of 4 nM and 3 nM, respectively[1][2].

In Vivo

Isoprenaline 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[1].

Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (10.26 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0518 mL 10.2589 mL 20.5179 mL
5 mM 0.4104 mL 2.0518 mL 4.1036 mL
10 mM 0.2052 mL 1.0259 mL 2.0518 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.5 mg/mL (1.03 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 0.5 mg/mL (1.03 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 0.5 mg/mL (1.03 mM); Clear solution

References
Molecular Weight

487.38

Formula

C₂₃H₁₆F₃N₃O₆

CAS No.

1488354-15-9

SMILES

O=C(N(C1=CC=C(N2C)C(OC2=O)=C1)C=C(C(O)=O)C3=O)N3[[email protected]]4C5=CC=CC(C(F)(F)F)=C5CC4

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

  • Molarity Calculator

  • Dilution Calculator

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This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
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Product Name:
Fulacimstat
Cat. No.:
HY-109059
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Fulacimstat

Cat. No.: HY-109059