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Fulacimstat

Cat. No. M22356
Fulacimstat Structure
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Biological Activity

Fulacimstat

Chemical Information
Molecular Weight 487.38
Formula C23H16F3N3O6
CAS Number 1488354-15-9
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Markus Weckmann, et al. Eur Respir J. COL4A3 is degraded in allergic asthma and degradation predicts response to anti-IgE therapy

[2] Peter Rossing, et al. Nephrol Dial Transplant. Effects of the chymase inhibitor fulacimstat in diabetic kidney disease-results from the CADA DIA trial

[3] Hans-Dirk Duengen, et al. Am Heart J. 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

[4] Hans-Dirk Dngen, et al. Clin Pharmacol Drug Dev. Safety and Tolerability of the Chymase Inhibitor Fulacimstat in Patients With Left Ventricular Dysfunction After Myocardial Infarction-Results of the CHIARA MIA 1 Trial

[5] Friederike Kanefendt, et al. Clin Pharmacol Drug Dev. Pharmacokinetics, Safety, and Tolerability of the Novel Chymase Inhibitor BAY 1142524 in Healthy Male Volunteers

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