Accueil>>Signaling Pathways>> Others>>Fulacimstat

Fulacimstat (Synonyms: BAY1142524)

Catalog No.GC19159

Le fulacimstat est un inhibiteur de chymase disponible par voie orale, avec des CI50 de 4, 3 nM pour l'enzyme chymase humaine et de hamster, respectivement.

Products are for research use only. Not for human use. We do not sell to patients.

Fulacimstat Chemical Structure

Cas No.: 1488354-15-9

Taille Prix Stock Qté
5mg
235,00 $US
En stock
10mg
335,00 $US
En stock
25mg
637,00 $US
En stock
50mg
1 105,00 $US
En stock
100mg
1 641,00 $US
En stock

Tel:(909) 407-4943 Email: sales@glpbio.com

Avis des clients

Based on customer reviews.

  • GlpBio Citations

    GlpBio Citations
  • Bioactive Compounds Premium Provider

    Bioactive Compounds Premium Provider

Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents Related Products

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.

Avis

Review for Fulacimstat

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

5 Star
100%
4 Star
0%
3 Star
0%
2 Star
0%
1 Star
0%
Review for Fulacimstat

GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.

Required fields are marked with *

You may receive emails regarding this submission. Any emails will include the ability to opt-out of future communications.