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AZD4831

Cat. No. M21420
AZD4831 Structure
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Biological Activity

AZD4831 is an oral covalent myeloperoxidase (MPO) inhibitor that is being developed for the study of heart failure.

Chemical Information
Molecular Weight 334.82
Formula C15H15ClN4OS
CAS Number 1933460-19-5
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] Ulrik Jurva, et al. Drug Metab Dispos. Biotransformation of the Novel Myeloperoxidase Inhibitor AZD4831 in Preclinical Species and Humans

[2] Tord Inghardt, et al. J Med Chem. Correction to "Discovery of AZD4831, a Mechanism-Based Irreversible Inhibitor of Myeloperoxidase, As a Potential Treatment for Heart Failure with Preserved Ejection Fraction"

[3] Tord Inghardt, et al. J Med Chem. Discovery of AZD4831, a Mechanism-Based Irreversible Inhibitor of Myeloperoxidase, As a Potential Treatment for Heart Failure with Preserved Ejection Fraction

[4] Karin Nelander, et al. Clin Transl Sci. Early Clinical Experience With AZD4831, A Novel Myeloperoxidase Inhibitor, Developed for Patients With Heart Failure With Preserved Ejection Fraction

[5] Li-Ming Gan, et al. Br J Clin Pharmacol. Safety, tolerability, pharmacokinetics and effect on serum uric acid of the myeloperoxidase inhibitor AZD4831 in a randomized, placebo-controlled, phase I study in healthy volunteers

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Keywords: AZD4831 supplier, inhibitors, activators

 
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