MPO-IN-1
Based on 1 Customer Validation
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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 98.07%
- CAS No.: 2471981-21-0
- Formule: C24H21ClN4
- Masse moléculaire:400.90
-
Stockage: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]
-
Activité biologique
-
Chemical Information
-
Solvant et solubilité
- Pureté et documentation
- Références
-
Help & FAQs
Activité biologique
Description
IC50 & Target
2.6 μM (in plasma MPO assay); 0.12 μM (in fluorescent MPO peroxidation assay)[1]
In Vivo
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.
Chemical Information
-
CAS No. 2471981-21-0
-
Appearance Solid
-
Masse moléculaire 400.90
-
Formule C24H21ClN4
-
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
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
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)
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)
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.
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:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
Pureté et documentation
-
Fiche technique (276 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Instruction de manipulation (2659 KB)
Références
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 |
MPO-IN-1 Related Classifications
HY-139915 Related Classifications
Powered by Bioz