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Fulacimstat (Synonyms: BAY1142524)

Catalog No.GC19159

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

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Fulacimstat Chemical Structure

Cas No.: 1488354-15-9

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5mg
$235.00
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10mg
$335.00
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25mg
$637.00
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50mg
$1,105.00
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100mg
$1,641.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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

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

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].

References:
[1]. 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.
[2]. Kanefendt F, et al. Pharmacokinetics, Safety, and Tolerability of the Novel Chymase Inhibitor BAY 1142524 in Healthy Male Volunteers. Clin Pharmacol Drug Dev. 2018 Jun 7.

Chemical Properties

Cas No. 1488354-15-9 SDF
Synonyms BAY1142524
Canonical SMILES O=C(N(C1=CC=C(N2C)C(OC2=O)=C1)C=C(C(O)=O)C3=O)N3[C@H]4C5=CC=CC(C(F)(F)F)=C5CC4
Formula C23H16F3N3O6 M.Wt 487.38
Solubility DMSO : 5 mg/mL (10.26 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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
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Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 6 reference(s) in Google Scholar.)

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