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
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
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- DC11394
- Product name
- Fulacimstat(BAY1142524)
- Purity
- >98%
- Packaging
- 100mg
- Price
- $950
- Updated
- 2021/12/16
- Product number
- DC11394
- Product name
- Fulacimstat(BAY1142524)
- Purity
- >98%
- Packaging
- 1g
- Price
- $3500
- Updated
- 2021/12/16
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
Raw materials
Preparation Products
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