2. Apoptosis Metabolic Enzyme/Protease
  3. Glutathione Peroxidase
  4. AZM198

AZM198 is an orally active myeloperoxidase (MPO) inhibitor. AZM198 irreversibly inactivates MPO (IC50=0.015 μM) via covalent binding to the heme prosthetic group, preferentially targets extracellular MPO activity, and reduces neutrophil extracellular trap formation, reactive oxygen species production and degranulation. AZM198 increases the fibrous cap thickness of atherosclerotic plaques, reduces lesion area, ameliorates hepatic steatosis and fibrosis in non-alcoholic steatohepatitis, and alleviates proteinuria and inflammatory infiltration associated with glomerulonephritis. AZM198 also decreases circulating levels of high-sensitivity Cardiac Troponin I and IL-1β, and mitigates endothelial cell injury. Therefore, AZM198 is suitable for research on various MPO-related diseases, including atherosclerotic cardiovascular disease, myocardial infarction, ischemic stroke, non-alcoholic steatohepatitis and crescentic glomerulonephritis.

For research use only. We do not sell to patients.

AZM198

AZM198 Chemical Structure

CAS No. : 1933460-23-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

AZM198 Related Antibodies

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Description

AZM198 is an orally active myeloperoxidase (MPO) inhibitor. AZM198 irreversibly inactivates MPO (IC50=0.015 μM) via covalent binding to the heme prosthetic group, preferentially targets extracellular MPO activity, and reduces neutrophil extracellular trap formation, reactive oxygen species production and degranulation. AZM198 increases the fibrous cap thickness of atherosclerotic plaques, reduces lesion area, ameliorates hepatic steatosis and fibrosis in non-alcoholic steatohepatitis, and alleviates proteinuria and inflammatory infiltration associated with glomerulonephritis. AZM198 also decreases circulating levels of high-sensitivity Cardiac Troponin I and IL-1β, and mitigates endothelial cell injury. Therefore, AZM198 is suitable for research on various MPO-related diseases, including atherosclerotic cardiovascular disease, myocardial infarction, ischemic stroke, non-alcoholic steatohepatitis and crescentic glomerulonephritis[1][2][3][4].
IC50 & Target

CYP3A4

19 μM (IC50)

In Vitro

AZM198 (10 μM) reduces reactive oxygen species production, neutrophil degranulation and neutrophil extracellular trap formation in human neutrophils prestimulated with TNFα and activated by PR3-ANCA, and attenuates the activity of enzymatically active myeloperoxidase in human neutrophils stimulated with PMA[1].
AZM198 (10 μM; 18 h) attenuates human neutrophil-mediated endothelial cell injury in a co-culture system of TNFα-prestimulated, PR3-ANCA-activated neutrophils and endothelial cells incubated for 18 hours[1].
AZM198 (10 μM; 2 h) reduces neutrophil extracellular trap (NET) formation in human neutrophils isolated from healthy donors, which is induced by Phorbol 12-myristate 13-acetate (HY-18739)[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

AZM198 Related Antibodies

Cell Viability Assay[1]

Cell Line: Endothelial Cell-Neutrophil Coculture
Concentration: 10 μM; with TNFα (2 ng/well)
Incubation Time: 18 h
Result: Attenuated human neutrophil-mediated endothelial cell injury.
In Vivo

AZM198 (133-400 μmol/kg; p.o.; once every 12 hours; for 7 consecutive days) reduces renal injury markers, including glomerular thrombosis, proteinuria, and plasma creatinine levels, in a mouse model of crescentic glomerulonephritis without enhancing adaptive immune responses[1].
AZM198 (133 μmol/kg; p.o.; twice daily; for 48 h) does not significantly reduce early glomerular neutrophil accumulation in a mouse model of crescentic glomerulonephritis[1].
AZM198 (400 μmol/kg; p.o.; twice daily; for 7 consecutive days) does not enhance antigen-specific T cell responses in a mouse adoptive transfer model[1].
AZM198 (400 μmol/kg; administered via gavage; twice daily; for 7 consecutive days) exerts no protective effects on either histological or biochemical indicators of disease in this mouse model of anti-neutrophil cytoplasmic antibody-associated vasculitis[2].
AZM198 (500 μmol/kg; oral administration; continuous administration via diet formulation; 26 weeks) increases the survival rate of male SR-BIΔCT/ΔCT/Ldlr-/- mice fed a Western diet by 92% (to a 63% survival rate), reduces the incidence of major adverse cardiovascular events by 57%-75%, and also attenuates cardiac fibrosis, liver injury, and inflammatory activity in atherosclerotic lesions[3].
AZM198 inhibits MPO activity in vulnerable atherosclerotic plaques, increases fibrous cap thickness by 65%, reduces intraplaque fibrin and hemosiderin, and promotes a more stable plaque phenotype in Apoe-/- mice with plaque instability induced by tandem stenosis[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 (female, 10-12 weeks old, average weight 25 g, injected intravenously with sheep nephrotoxic serum mixed 1:1 with LPS)[1]
Dosage: 133 μmol/kg
Administration: p.o.; twice a day; 48 hours
Result: Resulted in median Ly6g corrected total cell fluorescence (CTCF) of 26.5 (23-70.7) AU, representing a non-significant reduction in glomerular neutrophil infiltration compared to vehicle controls.
Animal Model: BALB/c (female)[1]
Dosage: 400 μmol/kg
Administration: p.o.; twice daily; 7 days
Result: Resulted in median frequency of CD44high CD4+ cells of 12.6% (11.8%-13.8%), representing no significant increase in activated total T cells compared to vehicle controls.
Resulted in median frequency of CD44high KJ+ CD4+ cells of 1.9% (1.64%-3.14%), representing no significant increase in activated ovalbumin-specific T cells compared to vehicle controls.
Animal Model: C57BL6/J mice (female, 8 weeks old, anti-neutrophil cytoplasmic antibody vasculitis model induced by G-CSF, anti-myeloperoxidase IgG, and lipopolysaccharide)[2]
Dosage: 400 μmol/kg per dose (total daily dose of 128 mg/kg)
Administration: oral gavage; twice daily; 7 days
Result: Showed no significant differences from controls in percentage of glomerular crescents, number of glomerular neutrophils, number of intraglomerular or periglomerular CD68-positive cells, serum creatinine levels at day 7, or urine albumin-creatinine ratios at day 6.
Molecular Weight

320.80

Formula

C14H13ClN4OS
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1NC(N(CC2=CC=C(C=C2CN)Cl)C3=C1NC=C3)=S
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 16.67 mg/mL (51.96 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1172 mL 15.5860 mL 31.1721 mL
5 mM 0.6234 mL 3.1172 mL 6.2344 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.67 mg/mL (5.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 1.67 mg/mL (5.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
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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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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
DMSO 1 mM 3.1172 mL 15.5860 mL 31.1721 mL 77.9302 mL
5 mM 0.6234 mL 3.1172 mL 6.2344 mL 15.5860 mL
10 mM 0.3117 mL 1.5586 mL 3.1172 mL 7.7930 mL
15 mM 0.2078 mL 1.0391 mL 2.0781 mL 5.1953 mL
20 mM 0.1559 mL 0.7793 mL 1.5586 mL 3.8965 mL
25 mM 0.1247 mL 0.6234 mL 1.2469 mL 3.1172 mL
30 mM 0.1039 mL 0.5195 mL 1.0391 mL 2.5977 mL
40 mM 0.0779 mL 0.3897 mL 0.7793 mL 1.9483 mL
50 mM 0.0623 mL 0.3117 mL 0.6234 mL 1.5586 mL
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AZM198 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AZM1981933460-23-1AZM 198AZM-198Glutathione Peroxidasehuman neutrophilsreactive oxygen speciescrescentic glomerulonephritisnonalcoholic steatohepatitisneutrophil degranulationatherosclerotic cardiovascular diseasemyeloperoxidasehaem prosthetic groupSR-BIΔCT/ΔCT/Ldlr?/? miceneutrophil extracellular trap formationInhibitorinhibitorinhibit

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