A chymase inhibitor
Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

Fulacimstat

Item No. 37731

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
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-pyrimidinecarboxylic acid
CAS Number
1488354-15-9
Synonyms
  • BAY-1142524
Molecular Formula
C23H16F3N3O6
Formula Weight
487.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
SMILES
O=C1N(C(C(C(O)=O)=CN1C2=CC=C(N(C(O3)=O)C)C3=C2)=O)[C@@]4([H])C5=CC=CC(C(F)(F)F)=C5CC4
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
InChi Key
JDARDSVOVYVQST-MRXNPFEDSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    1 mg

    $51

    Add

    5 mg

    $241

    Add

    10 mg

    $431

    Add

    25 mg

    $948

    Add
    Product Description

    Fulacimstat is an inhibitor of chymase (IC50s = 4 and 3 nM for the human and hamster enzyme, respectively).1 It reduces cardiac fibrosis induced by the β1-adrenergic receptor (B1-AR) and β2-AR agonist isoprenaline (isoproterenol; Item No. 15592) in hamsters when administered at doses of 1, 3, and 10 mg/kg. Fulacimstat (2 and 5 mg/kg per day) inhibits microembolism-induced decreases in left ventricular ejection fraction and increases in left ventricular end-systolic volume, decreases in plasma levels of N-terminal pro-brain natriuretic peptide (nt-proBNP), TGF-β1, and TNF-α, as well as the levels of interstitial fibrosis and the cross-sectional area of myocytes, a measure of myocyte hypertrophy, in a coronary microembolism-induced canine model of heart failure.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tinel, H., Zubov, D., Zimmermann, K., et al. Abstract 13624: A novel chymase inhibitor BAY 1142524 reduces fibrosis and improves cardiac function after myocardial infarction in hamster. Circulation 136(suppl. 1), A13624 (2017).

    2. Sabbah, H.N., Gupta, R.C., and Tinel, H. Abstract 11585: Long-term therapy with a chymase-1 inhibitor (BAY 1142524) improves left ventricular systolic function and prevents progressive chamber remodeling in dogs with heart failure. Circulation 136(suppl. 1), A11585 (2017).