2. Apoptosis Metabolic Enzyme/Protease
  3. Glutathione Peroxidase
  4. MPO-IN-1

MPO-IN-1 is a potent, orally active, and irreversible indole-containing inhibitor of myeloperoxidase (MPO). MPO-IN-1 has IC50s of 2.6 μM and 5.3 μM for MPO and thyroid peroxidase (TPO), respectively. MPO-IN-1 inhibits MPO activity in an acute mouse model of inflammation.

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MPO-IN-1 Chemical Structure

MPO-IN-1 Chemical Structure

CAS No. : 2471981-21-0

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5 mg USD 350 In-stock
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Based on 1 publication(s) in Google Scholar

MPO-IN-1 Related Antibodies

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Description

MPO-IN-1 is a potent, orally active, and irreversible indole-containing inhibitor of myeloperoxidase (MPO). MPO-IN-1 has IC50s of 2.6 μM and 5.3 μM for MPO and thyroid peroxidase (TPO), respectively. MPO-IN-1 inhibits MPO activity in an acute mouse model of inflammation[1].

IC50 & Target

2.6 μM (in plasma MPO assay); 0.12 μM (in fluorescent MPO peroxidation assay)[1]
In Vivo

MPO-IN-1 (compound 2) (5 and 90 mg/kg; p.o.; four hours post-Zymosan A administration) significantly reduces MPO activity in a mouse peritonitis model of acute inflammation[1].
Mouse pharmacokinetic parameter of MPO-IN-1[1].

Dose Vss
(L/kg)		 T1/2
(h)		 AUCinf
(nM•h) p.o.		 Cmax
(nM) p.o.		 PPB (%) F (%)
1/10 mg/kg i.v./p.o. 9.8 2.6 2486 502 99.6 61

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

Animal Model: Male C57BL/6J mice (mouse peritonitis model of acute inflammation)[1]
Dosage: 5 and 90 mg/kg
Administration: p.o. (four hours post-Zymosan A administration)
Result: Resulted in a ~50% reduction in the MPO activity at 90 mg/kg.
Molecular Weight

400.90

Formula

C24H21ClN4
CAS No.
Appearance

Solid

Color

Off-white to gray

SMILES

ClC1=C(C(C2=CC3=C(C=CN3)C=C2)=CN4C5=CC=C(CN(C)C)C=C5)C4=NC=C1
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 : 200 mg/mL (498.88 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 2.4944 mL 12.4719 mL 24.9439 mL
5 mM 0.4989 mL 2.4944 mL 4.9888 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.

  • Molarity Calculator

  • Dilution Calculator

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: ≥ 5 mg/mL (12.47 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
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 2.4944 mL 12.4719 mL 24.9439 mL 62.3597 mL
5 mM 0.4989 mL 2.4944 mL 4.9888 mL 12.4719 mL
10 mM 0.2494 mL 1.2472 mL 2.4944 mL 6.2360 mL
15 mM 0.1663 mL 0.8315 mL 1.6629 mL 4.1573 mL
20 mM 0.1247 mL 0.6236 mL 1.2472 mL 3.1180 mL
25 mM 0.0998 mL 0.4989 mL 0.9978 mL 2.4944 mL
30 mM 0.0831 mL 0.4157 mL 0.8315 mL 2.0787 mL
40 mM 0.0624 mL 0.3118 mL 0.6236 mL 1.5590 mL
50 mM 0.0499 mL 0.2494 mL 0.4989 mL 1.2472 mL
60 mM 0.0416 mL 0.2079 mL 0.4157 mL 1.0393 mL
80 mM 0.0312 mL 0.1559 mL 0.3118 mL 0.7795 mL
100 mM 0.0249 mL 0.1247 mL 0.2494 mL 0.6236 mL
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MPO-IN-1 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:

MPO-IN-12471981-21-0Glutathione PeroxidaseinflammationoralperoxidasemyeloperoxidaseMPOTPOindoleirreversibleInhibitorinhibitorinhibit

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