| Identification | Back Directory | [Name]
fulacimstat(BAY1142524) | [CAS]
1488354-15-9 | [Synonyms]
CS-2859
BAY1142524
fulacimstat(BAY1142524)
FULACIMSTAT;BAY 1142524;BAY-1142524;BAY1142524
5-Pyrimidinecarboxylic acid, 1-(2,3-dihydro-3-methyl-2-oxo-6-benzoxazolyl)-3-[(1R)-2,3-dihydro-4-(trifluoromethyl)-1H-inden-1-yl]-1,2,3,4-tetrahydro-2,4-dioxo- | [Molecular Formula]
C23H16F3N3O6 | [MDL Number]
MFCD31746878 | [MOL File]
1488354-15-9.mol | [Molecular Weight]
487.38 |
| Chemical Properties | Back Directory | [Boiling point ]
605.8±65.0 °C(Predicted) | [density ]
1.610±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:5.0(Max Conc. mg/mL);10.26(Max Conc. mM) | [form ]
Solid | [pka]
4.93±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Fulacimstat is an orally available chymase inhibitor, with IC50s of 4, 3 nM for human and hamster chymase enzyme, respectively. | [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]. | [storage]
Store at -20°C | [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. DOI:10.1002/cpdd.579 |
|
| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
Twochem Co.Ltd.
|
| Tel: |
021-58111628 15800915896 |
| Website: |
cn.twochem.com |
| Company Name: |
Cckinase, Inc.
|
| Tel: |
+1 (732)236-3202 |
| Website: |
www.cckinase.com |
|