fulacimstat(BAY1142524)

Product Name: fulacimstat(BAY1142524)
CAS No.: 1488354-15-9
Chemical Name: fulacimstat(BAY1142524)
Synonyms: CS-2859;BAY1142524;fulacimstat(BAY1142524);Fulacimstat, 10 mM in DMSO;FULACIMSTAT;BAY 1142524;BAY-1142524;BAY1142524;Fulacimstat,inhibit,BAY 1142524,Inhibitor,BAY-1142524;Fulacimstat,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-5-;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-;(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-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-1-yl]-1,2,3,4-tetrahydropyrimidine-5-carboxylic acid
CBNumber: CB34671058
Molecular Formula: C23H16F3N3O6
Formula Weight: 487.38
MOL File: 1488354-15-9.mol

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fulacimstat(BAY1142524) Property

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
InChIKey: JDARDSVOVYVQST-MRXNPFEDSA-N
SMILES: C1(=O)N(C2C=C3OC(=O)N(C)C3=CC=2)C=C(C(O)=O)C(=O)N1[C@H]1C2=C(C(C(F)(F)F)=CC=C2)CC1

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

DC Chemicals

Product number: DC11394
Product name: Fulacimstat(BAY1142524)
Purity: >98%
Packaging: 100mg
Price: $950
Updated: 2021/12/16

DC Chemicals

Product number: DC11394
Product name: Fulacimstat(BAY1142524)
Purity: >98%
Packaging: 1g
Price: $3500
Updated: 2021/12/16

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fulacimstat(BAY1142524) Chemical Properties,Usage,Production

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].

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

fulacimstat(BAY1142524) Preparation Products And Raw materials

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fulacimstat(BAY1142524) Suppliers

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1488354-15-9, fulacimstat(BAY1142524)Related Search:

fulacimstat(BAY1142524)

BAY1142524

FULACIMSTAT;BAY 1142524;BAY-1142524;BAY1142524

CS-2859

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-

Fulacimstat,inhibit,BAY 1142524,Inhibitor,BAY-1142524

Fulacimstat,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-5-

(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-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-1-yl]-1,2,3,4-tetrahydropyrimidine-5-carboxylic acid

Fulacimstat, 10 mM in DMSO

1488354-15-9

C23H16F3N3O6