(R)-MMP408
Based on 1 Customer Validation
(R)-MMP408 is an isomer of MMP408 (HY-12093). MMP408 is an orally active MMP-12 inhibitor (IC50=2.0 nM for hMMP-12) that effectively interferes with the epithelial-mesenchymal transition (EMT) process. MMP408 significantly upregulates the expression of E-cadherin in nasal epithelial cells, while inhibiting mesenchymal markers such as vimentin, α-smooth muscle actin and fibronectin, thereby reversing the EMT phenotype. MMP408 is used in studies of airway remodeling-related diseases, including chronic rhinosinusitis with nasal polyps, chronic obstructive pulmonary disease (COPD) and asthma.
For research use only. We do not sell to patients.
- Purity: 99.63%
- CAS No.: 1258003-93-8
- Formula: C19H20N2O7S
- Molecular Weight:420.44
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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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human MMP-12 2 nM (IC50) |
MMP408 (10 nM) inhibits MMP-12-induced epithelial-mesenchymal transition in primary nasal epithelial cells by restoring E-cadherin expression and reducing mesenchymal marker expression[1].
MMP408 (10 nM) inhibits MMP-12-induced epithelial-mesenchymal transition and restores epithelial barrier function in air-liquid interface nasal epithelial cell cultures[1].
MMP408 (4-25 nM; 15 min pre-substrate incubation at room temperature) potently and selectively inhibits human MMP-12 catalytic domain in vitro with an IC50 of 18.9 nM, while showing minimal activity against other tested MMP family members at the same concentrations[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Oral administration of MMP408 exerts efficacy in alleviating recombinant human MMP-12-induced pulmonary inflammation in C57BL/6 mice, with a favorable dose-effect relationship[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1258003-93-8
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Appearance Solid
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Molecular Weight 420.44
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Formula C19H20N2O7S
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Color White to off-white
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SMILES
CC(C)[C@H](C(O)=O)NS(=O)(C1=CC=C2C(OC3=CC=C(NC(OC)=O)C=C23)=C1)=O
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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 (237.85 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.95 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 (5.95 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 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.
Purity & Documentation
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Data Sheet (275 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 | 2.3785 mL | 11.8923 mL | 23.7846 mL | 59.4615 mL |
| 5 mM | 0.4757 mL | 2.3785 mL | 4.7569 mL | 11.8923 mL | |
| 10 mM | 0.2378 mL | 1.1892 mL | 2.3785 mL | 5.9462 mL | |
| 15 mM | 0.1586 mL | 0.7928 mL | 1.5856 mL | 3.9641 mL | |
| 20 mM | 0.1189 mL | 0.5946 mL | 1.1892 mL | 2.9731 mL | |
| 25 mM | 0.0951 mL | 0.4757 mL | 0.9514 mL | 2.3785 mL | |
| 30 mM | 0.0793 mL | 0.3964 mL | 0.7928 mL | 1.9821 mL | |
| 40 mM | 0.0595 mL | 0.2973 mL | 0.5946 mL | 1.4865 mL | |
| 50 mM | 0.0476 mL | 0.2378 mL | 0.4757 mL | 1.1892 mL | |
| 60 mM | 0.0396 mL | 0.1982 mL | 0.3964 mL | 0.9910 mL | |
| 80 mM | 0.0297 mL | 0.1487 mL | 0.2973 mL | 0.7433 mL | |
| 100 mM | 0.0238 mL | 0.1189 mL | 0.2378 mL | 0.5946 mL |