| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
MMP-2 6.6 μM (IC50) MMP-13 1.8 μM (IC50) MMP-1 10 μM (IC50) MMP-9 13 μM (IC50)
MMPI-1154 targets matrix metalloproteinase-2 (MMP-2), a zinc-dependent endopeptidase involved in extracellular matrix remodeling. MMP-2 is implicated in various pathological processes including tissue injury, inflammation, and cardiovascular disease. MMPI-1154 also inhibits MMP-13, MMP-1, and MMP-9 with varying potencies. By inhibiting MMP-2 and other MMPs, the compound reduces extracellular matrix degradation and protects cardiac tissue from injury. |
|---|---|
| ln Vitro |
MMP-2 enzyme isolated from rat heart is inhibited in vitro by MMPI-1154 (1-100 μM), with 100% inhibition observed at concentrations of 100 μM[1]. In an ex vivo model for acute myocardial infarction, MMPI-1154 (1 μM) significantly reduces infarct size and exhibits strong cardio-cytoprotecion[1].
In vitro, MMPI-1154 demonstrates potent inhibition of MMP-2 with an IC50 of 6.6 µM. It also inhibits MMP-13 with an IC50 of 1.8 µM, MMP-1 with an IC50 of 10 µM, and MMP-9 with an IC50 of 13 µM. The compound shows concentration-dependent inhibition of MMP activity in biochemical assays using purified enzymes. MMPI-1154 exhibits excellent cardio-cytoprotective properties, making it a promising candidate for acute myocardial infarction research. |
| ln Vivo |
In vivo, MMPI-1154 has been evaluated in ex vivo models of acute myocardial infarction. At a concentration of 1 µM, the compound significantly decreased infarct size in an ex vivo model. This cardioprotective effect supports the compound's potential as a therapeutic agent for acute myocardial infarction. Detailed efficacy studies in animal models have been reported, demonstrating the compound's ability to protect cardiac tissue from ischemic injury.
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| Enzyme Assay |
The in vitro enzyme inhibition assay for MMPI-1154 typically involves measuring MMP-2, MMP-13, MMP-1, or MMP-9 activity using a fluorogenic peptide substrate. Purified enzyme is incubated with varying concentrations of MMPI-1154 (0.001-100 µM) in assay buffer (e.g., Tris-HCl, pH 7.5, containing calcium and zinc ions) at 37°C for 30-60 minutes. The reaction is initiated by adding the substrate, and fluorescence is measured continuously. IC50 values are calculated from dose-response curves.
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| Cell Assay |
For in vitro cell-based assays, cardiac cells or other relevant cell lines are cultured and treated with MMPI-1154 at concentrations ranging from 0.1-100 µM for 24-72 hours. MMP activity is measured in cell lysates or conditioned media using zymography or activity assays. Cell viability is assessed using MTT or CCK-8 assays. Cardioprotective effects are evaluated by measuring markers of cell injury and apoptosis.
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| Animal Protocol |
In vivo animal studies for MMPI-1154 are conducted using models of acute myocardial infarction, such as ischemia-reperfusion injury in rodents. MMPI-1154 is administered via intravenous injection or oral gavage at doses ranging from 1-50 mg/kg prior to or after ischemic injury. Infarct size is measured by TTC staining or histology. Cardiac function is assessed by echocardiography. MMP activity and tissue injury markers are measured in cardiac tissue.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of MMPI-1154 have been partially characterized. The molecular weight is 445.49 g/mol and the molecular formula is C₂₆H₂₄FN₃O₃. The compound is supplied as a high-purity solid. Detailed pharmacokinetic parameters such as bioavailability, half-life, and protein binding have not been extensively reported. Stability in solution may be limited and fresh solutions should be prepared for each experiment.
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| Toxicity/Toxicokinetics |
Toxicology data for MMPI-1154 are limited. As a research compound, it has not been systematically evaluated for safety. The compound's mechanism of MMP inhibition suggests potential effects on tissue remodeling and wound healing, which would require careful safety assessment. Standard toxicological endpoints including cell viability, genotoxicity, and organ toxicity should be evaluated. The compound is intended for research use only.
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| References | |
| Additional Infomation |
MMPI-1154 is a novel cardio-cytoprotective MMP-2 inhibitor with an IC50 of 6.6 µM. It also inhibits MMP-13 (1.8 µM), MMP-1 (10 µM), and MMP-9 (13 µM). The compound significantly decreases infarct size in ex vivo models of acute myocardial infarction and is a promising lead candidate for the treatment of acute myocardial infarction. MMPI-1154 is intended for research use only.
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| Molecular Formula |
C26H24FN3O3
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|---|---|
| Molecular Weight |
445.485469818115
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| Exact Mass |
445.18
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| CAS # |
1382722-47-5
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| PubChem CID |
68027884
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| Appearance |
White to yellow solid powder
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| LogP |
2.1
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
33
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| Complexity |
587
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1C=CC(=CC=1)CN(CC1=NC=C(C(=O)O)N1)CC1C=CC(=CC=1)OCC1C=CC=CC=1
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| InChi Key |
QLTNFRCPUOPISS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H24FN3O3/c27-22-10-6-19(7-11-22)15-30(17-25-28-14-24(29-25)26(31)32)16-20-8-12-23(13-9-20)33-18-21-4-2-1-3-5-21/h1-14H,15-18H2,(H,28,29)(H,31,32)
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| Chemical Name |
2-[[(4-fluorophenyl)methyl-[(4-phenylmethoxyphenyl)methyl]amino]methyl]-1H-imidazole-5-carboxylic acid
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO: 83.33 mg/mL (187.05 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.67 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.67 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 can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.67 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2447 mL | 11.2236 mL | 22.4472 mL | |
| 5 mM | 0.4489 mL | 2.2447 mL | 4.4894 mL | |
| 10 mM | 0.2245 mL | 1.1224 mL | 2.2447 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.
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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