MEDS433
Based on 1 Customer Validation
MEDS433 is a potent inhibitor of human dihydroorotate dehydrogenase (hDHODH) with an IC50 of 1.2 nM. MEDS433 exerts a potent antiviral activity against RSV-A and RSV-B in the one-digit nanomolar range. MEDS433 induces the expression of antiviral proteins encoded by interferon stimulated genes (ISGs) able to reduce RSV replication.
For research use only. We do not sell to patients.
- Purity: 99.51%
- CAS No.: 2241027-61-0
- Formula: C20H11F4N3O2
- Molecular Weight:401.31
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Jurkat | IC50 |
0.75 μM
Compound: 4
|
Antiproliferative activity against human Jurkat T cells assessed as DNA content after 72 hrs by Hoechst 33258 dye-based fluorescence assay
Antiproliferative activity against human Jurkat T cells assessed as DNA content after 72 hrs by Hoechst 33258 dye-based fluorescence assay
|
[PMID: 29939742] |
| Jurkat | IC50 |
68.69 μM
Compound: 4
|
Antiproliferative activity against human Jurkat T cells assessed as DNA content after 72 hrs in presence of exogenous uridine by Hoechst 33258 dye-based fluorescence assay
Antiproliferative activity against human Jurkat T cells assessed as DNA content after 72 hrs in presence of exogenous uridine by Hoechst 33258 dye-based fluorescence assay
|
[PMID: 29939742] |
| PBMC | IC50 |
0.78 μM
Compound: 4
|
Immunosuppressive activity against human PBMC assessed as inhibition of PHA-stimulated cell proliferation preincubated for 2 hrs followed by PHA stimulation for 72 hrs by Hoechst 33258 dye-based fluorescence assay
Immunosuppressive activity against human PBMC assessed as inhibition of PHA-stimulated cell proliferation preincubated for 2 hrs followed by PHA stimulation for 72 hrs by Hoechst 33258 dye-based fluorescence assay
|
[PMID: 29939742] |
| PBMC | IC50 |
57.15 μM
Compound: 4
|
Immunosuppressive activity against human PBMC assessed as inhibition of PHA-stimulated cell proliferation preincubated for 2 hrs followed by PHA stimulation for 72 hrs in presence of exogenous uridine by Hoechst 33258 dye-based fluorescence assay
Immunosuppressive activity against human PBMC assessed as inhibition of PHA-stimulated cell proliferation preincubated for 2 hrs followed by PHA stimulation for 72 hrs in presence of exogenous uridine by Hoechst 33258 dye-based fluorescence assay
|
[PMID: 29939742] |
| THP-1 | EC50 |
0.0397 μM
Compound: 1
|
Induction of cell differentiation in human THP-1 cells assessed as CD14 expression after 3 days by flow cytometric analysis
Induction of cell differentiation in human THP-1 cells assessed as CD14 expression after 3 days by flow cytometric analysis
|
[PMID: 33844533] |
| THP-1 | EC50 |
0.0723 μM
Compound: 1
|
Induction of apoptosis in human THP-1 cells after 3 days by Annexin-V-FITC staining based flow cytometry
Induction of apoptosis in human THP-1 cells after 3 days by Annexin-V-FITC staining based flow cytometry
|
[PMID: 33844533] |
| THP-1 | EC50 |
40 nM
Compound: MEDS433
|
Induction of cell differentiation in human THP-1 cells measured for 2 days by flow cytometric analysis
Induction of cell differentiation in human THP-1 cells measured for 2 days by flow cytometric analysis
|
[PMID: 36162075] |
| THP-1 | EC50 |
72 nM
Compound: MEDS433
|
Induction of apoptosis in human THP-1 cells measured after 3 days by Annexin-V-FITC staining based FACS analysis
Induction of apoptosis in human THP-1 cells measured after 3 days by Annexin-V-FITC staining based FACS analysis
|
[PMID: 36162075] |
| U-937 | EC50 |
0.026 μM
Compound: 1
|
Induction of cell differentiation in human U-937 cells assessed as CD11b expression after 3 days by flow cytometric analysis
Induction of cell differentiation in human U-937 cells assessed as CD11b expression after 3 days by flow cytometric analysis
|
[PMID: 33844533] |
| U-937 | EC50 |
0.0404 μM
Compound: 1
|
Induction of apoptosis in human U-937 cells after 3 days by Annexin-V-FITC staining based flow cytometry
Induction of apoptosis in human U-937 cells after 3 days by Annexin-V-FITC staining based flow cytometry
|
[PMID: 33844533] |
| U-937 | EC50 |
26 nM
Compound: MEDS433
|
Induction of cell differentiation in human U-937 cells measured for 2 days by flow cytometric analysis
Induction of cell differentiation in human U-937 cells measured for 2 days by flow cytometric analysis
|
[PMID: 36162075] |
| U-937 | EC50 |
40 nM
Compound: MEDS433
|
Induction of apoptosis in human U-937 cells measured after 3 days by Annexin-V-FITC staining based FACS analysis
Induction of apoptosis in human U-937 cells measured after 3 days by Annexin-V-FITC staining based FACS analysis
|
[PMID: 36162075] |
Chemical Information
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CAS No. 2241027-61-0
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Appearance Solid
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Molecular Weight 401.31
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Formula C20H11F4N3O2
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Color White to off-white
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SMILES
O=C(C1=C2C=CC=CN2N=C1O)NC3=C(F)C(F)=C(C4=CC=CC=C4)C(F)=C3F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (249.18 mM; Need ultrasonic; 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)
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.
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.
Purity & Documentation
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Data Sheet (277 KB)
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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)
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Handling Instructions (2659 KB)
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 | 2.4918 mL | 12.4592 mL | 24.9184 mL | 62.2960 mL |
| 5 mM | 0.4984 mL | 2.4918 mL | 4.9837 mL | 12.4592 mL | |
| 10 mM | 0.2492 mL | 1.2459 mL | 2.4918 mL | 6.2296 mL | |
| 15 mM | 0.1661 mL | 0.8306 mL | 1.6612 mL | 4.1531 mL | |
| 20 mM | 0.1246 mL | 0.6230 mL | 1.2459 mL | 3.1148 mL | |
| 25 mM | 0.0997 mL | 0.4984 mL | 0.9967 mL | 2.4918 mL | |
| 30 mM | 0.0831 mL | 0.4153 mL | 0.8306 mL | 2.0765 mL | |
| 40 mM | 0.0623 mL | 0.3115 mL | 0.6230 mL | 1.5574 mL | |
| 50 mM | 0.0498 mL | 0.2492 mL | 0.4984 mL | 1.2459 mL | |
| 60 mM | 0.0415 mL | 0.2077 mL | 0.4153 mL | 1.0383 mL | |
| 80 mM | 0.0311 mL | 0.1557 mL | 0.3115 mL | 0.7787 mL | |
| 100 mM | 0.0249 mL | 0.1246 mL | 0.2492 mL | 0.6230 mL |