Mitiperstat

Mitiperstat (AZD4831) is an effective oral inhibitor of myeloperoxidase (MPO) . Mitiperstat inhibits MPO and thyroid peroxidase (TPO) with IC50s of 1.5 nM and 0.69 μM. Mitiperstat exhibits a weak inhibitory activity against CYP3A4 with an IC50 of 6 μM. Mitiperstat can reduce inflammation and improve microvascular function, and it can be used in studies related to heart failure, preserved or mildly reduced ejection fraction, non-alcoholic fatty liver disease, and chronic obstructive pulmonary disease[1][2][3][4].

Product Specifications

CAS Number

[1933460-19-5]

Product Name Alternative

AZD4831

UNSPSC

12352005

Hazard Statement

H302, H314

Target

Cytochrome P450; Glutathione Peroxidase

Type

Reference compound

Related Pathways

Apoptosis; Metabolic Enzyme/Protease

Applications

Neuroscience-Neuromodulation

Field of Research

Inflammation/Immunology; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/mitiperstat.html

Purity

99.12

Solubility

1 M HCl : 50 mg/mL (adjust pH to 1 with 1 M HCl) |DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(NC1=S)C(NC=C2)=C2N1CC3=C(C=C(C=C3)Cl)[C@H](N)C

Molecular Formula

C15H15ClN4OS

Molecular Weight

334.82

Precautions

H302, H314

References & Citations

[1]Joanna Parkinson, et al. The myeloperoxidase inhibitor mitiperstat (AZD4831) does not prolong the QT interval at expected therapeutic doses. Pharmacol Res Perspect. 2024 Apr;12 (2) :e1184.|[2]Lars H Lund, et al. Rationale and design of ENDEAVOR: A sequential phase 2b-3 randomized clinical trial to evaluate the effect of myeloperoxidase inhibition on symptoms and exercise capacity in heart failure with preserved or mildly reduced ejection fraction. Eur J Heart Fail. 2023 Sep;25 (9) :1696-1707.|[3]Carolyn S P Lam, et al. Myeloperoxidase Inhibition in Heart Failure With Preserved or Mildly Reduced Ejection Fraction: SATELLITE Trial Results. J Card Fail. 2024 Jan;30 (1) :104-110.|[4]Inghardt T, et al., Discovery of AZD4831, a Mechanism-Based Irreversible Inhibitor of Myeloperoxidase, As a Potential Treatment for Heart Failure with Preserved Ejection Fraction. J Med Chem. 2022 Sep 8;65 (17) :11485-11496.