Mitiperstat-d3
Mitiperstat-d3 (AZD4831-d3) is the deuterated -labeled Mitiperstat (HY-145581).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.
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- Formule: C15H12D3ClN4OS
- Masse moléculaire:337.84
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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Animal Model:Mouse zymosan-induced neutrophilic peritonitis models[4]
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Dosage:0.01-10 μmol/kg (3.3482 ng/kg-3.3482 μg/kg)
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Administration:po, single dose
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Result:Inhibited the peroxidase activity in mouse peritoneal lavage fluid.
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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Unlabeled Cas 1933460-19-5
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Masse moléculaire 337.84
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Formule C15H12D3ClN4OS
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SMILES
O=C(NC1=S)C(NC=C2)=C2N1CC3=C(C=C(C=C3)Cl)[C@H](N)C([2H])([2H])[2H]
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Synonyms
AZD4831-d3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Mitiperstat-d3 Related Classifications
HY-145581S Related Classifications
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