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(R)-MMP408

Cat No.:V121945 Purity: ≥98%
(R)-MMP408 is an orally effective MMP-12 inhibitor (IC50 for hMMP-12 = 2.0 nM) that effectively interferes with the epithelial-mesenchymal transition (EMT) process.
(R)-MMP408
(R)-MMP408 Chemical Structure CAS No.: 1258003-93-8
Product category: MMP
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
Other Sizes

Other Forms of (R)-MMP408:

  • MMP408
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
(R)-MMP408 is an orally effective MMP-12 inhibitor (IC50 for hMMP-12 = 2.0 nM) that effectively interferes with the epithelial-mesenchymal transition (EMT) process. (R)-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. (R)-MMP408 has been used in studies of airway remodeling-related diseases, including chronic sinusitis with nasal polyps, chronic obstructive pulmonary disease (COPD), and asthma.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
(R)-MMP408 (10 nM) inhibited MMP-12-induced epithelial-mesenchymal transition in primary nasal epithelial cells by restoring the expression of E-cadherin and reducing the expression of mesenchymal markers [1]. (R)-MMP408 (10 nM) inhibited MMP-12-induced epithelial-mesenchymal transition and restored epithelial barrier function in air-liquid interface nasal epithelial cell cultures [1]. MMP408 (4-25 nM; substrate pre-incubation at room temperature for 15 min) effectively and selectively inhibited the catalytic domain of human MMP-12 in vitro with an IC50 of 18.9 nM, while exhibiting very low activity against other tested MMP family members at the same concentration [2].
ln Vivo
(R)-MMP408 (intraperitoneal injection; once daily; for 7 days) protected C57BL/6 mice from elastase-induced emphysema damage, with an MLI value comparable to that of unstimulated control mice [2]. Oral administration of (R)-MMP408 effectively reduced recombinant human MMP-12-induced lung inflammation in C57BL/6 mice with a good dose-response relationship [3].
References

[1]. Matrix metalloproteinase-12 by M2 macrophages induced epithelial to mesenchymal transition in chronic rhinosinusitis with nasal polyps[J]. Plos one, 2024, 19(12): e0313097.

[2]. Therapeutic targeting of MMP-12 for the treatment of chronic obstructive pulmonary disease[J]. Journal of medicinal chemistry, 2020, 63(21): 12911-12920.

[3]. Discovery of potent and selective matrix metalloprotease 12 inhibitors for the potential treatment of chronic obstructive pulmonary disease (COPD). Bioorg Med Chem Lett. 2012;22(1):138-143.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C19H20N2O7S
Molecular Weight
420.44
CAS #
1258003-93-8
Related CAS #
MMP408
Appearance
White to off-white solid
SMILES
CC(C)[C@H](C(O)=O)NS(=O)(C1=CC=C2C(OC3=CC=C(NC(OC)=O)C=C23)=C1)=O
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~100 mg/mL (~237.85 mM; with sonication)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.95 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you canAdd 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of physiological saline: Dissolve 0.9 g of sodium chloride in double-distilled water and dilute to 100 mL to obtain clear physiological saline.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (5.95 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you canAdd 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD saline (4°C, store for one week): Dissolve 2 g of SBE-β-CD powder in 10 mL of saline until completely dissolved and clear.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (5.95 mM)(saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you canAdd 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.3785 mL 11.8923 mL 23.7846 mL
5 mM 0.4757 mL 2.3785 mL 4.7569 mL
10 mM 0.2378 mL 1.1892 mL 2.3785 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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