Fulacimstat

SKU: orb1296254

Description

Fulacimstat (BAY1142524) is a potent and selective chymase inhibitor, demonstrating IC50 values of 3 nM and 4 nM against hamster and human enzymes, respectively. This small molecule is a valuable research tool for investigating chymase roles in cardiovascular and fibrotic diseases in both in vitro and in vivo experimental models.

Research Area

Protein Biochemistry

Key Properties

• CAS Number: 1488354-15-9
• MW: 487.38
• Purity: 99.77% (May vary between batches)
• Formula: C₂₃H₁₆F₃N₃O₆
• SMILES: Cn1c2ccc(cc2oc1=O)-n1cc(C(O)=O)c(=O)n([C@@H]2CCc3c2cccc3C(F)(F)F)c1=O
• Target: Proteasome,Others
• Solubility: DMSO:5 mg/mL (10.26 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.05 mM)

Bioactivity

• Target IC50:
  Hamster chymase enzyme:3 nM|Chymase:4 nM
• In Vivo:
  Isoprenaline induces cardiac fibrosis (24.4%) in hamsters, which is reduced dose-dependently by Fulacimstat (16.4%, 12.4%, 10.9% at 1, 3 and 10 mg/kg respectively). Four weeks after MI, hamster hearts show increased end-diastolic pressure and reduce contractility and relaxation. Compared to placebo (19.3±2 mmHg), Fulacimstat at 10 mg/kg reduces significantly the end-diastolic pressure (13.2±1.4 mmHg) without any effects on blood pressure or heart rate. Moreover, treatment with Fulacimstat reduces the fibrotic area and improves the cardiac response to adrenergic stimulation .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

chymase, BAY 1142524, BAY1142524, BAY-1142524, Fulacimstat, Inhibitor, inhibit

Compound Identifiers

PubChem CID

91758792