Mitiperstat
Based on 1 publication(s) in Google Scholar
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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- Purity: 99.12%
- CAS No.: 1933460-19-5
- 화학식: C15H15ClN4OS
- 분자량:334.82
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Mitiperstat
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Biological Activity
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1933460-19-5
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Appearance Solid
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분자량 334.82
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화학식 C15H15ClN4OS
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Color White to light pink
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SMILES
O=C(NC1=S)C(NC=C2)=C2N1CC3=C(C=C(C=C3)Cl)[C@H](N)C
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Synonyms
AZD4831
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
용액&용해도
DMSO : 100 mg/mL (298.67 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
1 M HCl : 50 mg/mL (149.33 mM; adjust pH to 1 with 1 M HCl)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.47 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (7.47 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (278 KB)
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SDS (554 KB)
- English - EN (554 KB)
- Français - FR (554 KB)
- Deutsch - DE (554 KB)
- Norwegian - NO (554 KB)
- Español - ES (554 KB)
- Swedish - SV (554 KB)
- Italian - IT (554 KB)
- Korean - KR (554 KB)
- Portuguese - PT (554 KB)
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Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| 1 M HCl / DMSO | 1 mM | 2.9867 mL | 14.9334 mL | 29.8668 mL | 74.6670 mL |
| 5 mM | 0.5973 mL | 2.9867 mL | 5.9734 mL | 14.9334 mL | |
| 10 mM | 0.2987 mL | 1.4933 mL | 2.9867 mL | 7.4667 mL | |
| 15 mM | 0.1991 mL | 0.9956 mL | 1.9911 mL | 4.9778 mL | |
| 20 mM | 0.1493 mL | 0.7467 mL | 1.4933 mL | 3.7333 mL | |
| 25 mM | 0.1195 mL | 0.5973 mL | 1.1947 mL | 2.9867 mL | |
| 30 mM | 0.0996 mL | 0.4978 mL | 0.9956 mL | 2.4889 mL | |
| 40 mM | 0.0747 mL | 0.3733 mL | 0.7467 mL | 1.8667 mL | |
| 50 mM | 0.0597 mL | 0.2987 mL | 0.5973 mL | 1.4933 mL | |
| 60 mM | 0.0498 mL | 0.2489 mL | 0.4978 mL | 1.2444 mL | |
| 80 mM | 0.0373 mL | 0.1867 mL | 0.3733 mL | 0.9333 mL | |
| 100 mM | 0.0299 mL | 0.1493 mL | 0.2987 mL | 0.7467 mL |
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