| Cas No.: | 1488354-15-9 |
| Chemical Name: | Fulacimstat |
| Synonyms: | Fulacimstat;VIR72PP4ZU;BAY1142524;Fulacimstat [INN];Fulacimstat; BAY1142524;Fulacimstat(BAY 1142524);DB15085;1-yl]-1,2,3,4-tetrahydropyrimidine-5-carboxylic acid;1-(3-methyl-2-oxo-2,3-dihydro-1,3-benzoxazol-6-yl)-;2,4-dioxo-3-[(1R)-4-(trifluoromethyl)-2,3-dihydro-1H-inden-;(R)-1-(3-methyl-2-oxo-2,3-dihydrobenzo[d]oxazol-6-yl)-2,4-dioxo-3-(4-(trifluoromethyl)-2,3-dihydro-1H-inden-1-yl)-1,2,3,4-te |
| SMILES: | FC(C1=C([H])C([H])=C([H])C2=C1C([H])([H])C([H])([H])[C@@]2([H])N1C(C(C(=O)O[H])=C([H])N(C2C([H])=C([H])C3=C(C=2[H])OC(N3C([H])([H])[H])=O)C1=O)=O)(F)F |
| Formula: | C23H16F3N3O6 |
| M.Wt: | 487.3849 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | 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]. |
| In Vitro: | Fulacimstat inhibits human and hamster chymase enzyme with IC50s of 4 nM and 3 nM, respectively[1][2]. |
| 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. |
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COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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