Synonym
Fulacimstat; BAY1142524; BAY-1142524; BAY 1142524;
IUPAC/Chemical Name
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
InChi Key
JDARDSVOVYVQST-MRXNPFEDSA-N
InChi Code
InChI=1S/C23H16F3N3O6/c1-27-17-7-5-11(9-18(17)35-22(27)34)28-10-14(20(31)32)19(30)29(21(28)33)16-8-6-12-13(16)3-2-4-15(12)23(24,25)26/h2-5,7,9-10,16H,6,8H2,1H3,(H,31,32)/t16-/m1/s1
SMILES Code
O=C(C1=CN(C2=CC=C3N(C)C(OC3=C2)=O)C(N([C@@H]4CCC5=C4C=CC=C5C(F)(F)F)C1=O)=O)O
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMSO |
5.0 |
10.26 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
487.39
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
1: Düngen HD, Kober L, Nodari S, Schou M, Otto C, Becka M, Kanefendt F, Winkelmann BR, Gislason G, Richard F, Nielsen OW, Gheorghiade M, Senni M. Safety and Tolerability of the Chymase Inhibitor Fulacimstat in Patients With Left Ventricular Dysfunction After Myocardial Infarction-Results of the CHIARA MIA 1 Trial. Clin Pharmacol Drug Dev. 2019 Oct;8(7):942-951. doi: 10.1002/cpdd.633. Epub 2018 Nov 19. PMID: 30452784.
2: Duengen HD, Kim RJ, Zahger D, Orvin K, Kornowski R, Admon D, Kettner J, Shimony A, Otto C, Becka M, Kanefendt F, Romo AI, Hasin T, Ostadal P, Rojas GC, Senni M; GROUP investigators of the CHIARA MIA 2 trial. Effects of the chymase inhibitor fulacimstat on adverse cardiac remodeling after acute myocardial infarction-Results of the Chymase Inhibitor in Adverse Remodeling after Myocardial Infarction (CHIARA MIA) 2 trial. Am Heart J. 2020 Jun;224:129-137. doi: 10.1016/j.ahj.2020.01.012. Epub 2020 Jan 25. PMID: 32375104.
3: Kanefendt F, Thuß U, Becka M, Boxnick S, Berse M, Schultz A, Otto C. Pharmacokinetics, Safety, and Tolerability of the Novel Chymase Inhibitor BAY 1142524 in Healthy Male Volunteers. Clin Pharmacol Drug Dev. 2019 May;8(4):467-479. doi: 10.1002/cpdd.579. Epub 2018 Jun 7. PMID: 29878583.
