| 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-7 (IC50 = 2.8 nM). It is a potent and selective inhibitor of MMP-7, a protease involved in extracellular matrix degradation, tissue remodeling, and the activation of other proteases and growth factors.
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| ln Vitro |
MMP-7-IN-3 is a potent and selective inhibitor of MMP-7 with an IC50 of 2.8 nM. Its high potency makes it an even more powerful tool than MMP-7-IN-1 (IC50 = 10 nM) for studying this protease. It is a specific compound for investigating the role of MMP-7 in disease processes.
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| ln Vivo |
In vivo, MMP-7-IN-3 has been shown to suppress the progression of renal fibrosis in a mouse model of unilateral ureteral obstruction (UUO). This demonstrates that inhibition of MMP-7 can slow or halt the development of fibrosis in the kidney, providing proof-of-concept that MMP-7 is a viable therapeutic target for fibrotic diseases. Its in vivo efficacy opens up new avenues for treating such conditions.
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| Enzyme Assay |
For non-cellular assays, recombinant human MMP-7 is incubated with a fluorogenic FRET peptide substrate in a standard MMP assay buffer (e.g., 50 mM Tris-HCl, pH 7.5, 10 mM CaCl2, 150 mM NaCl, 0.05% Brij-35). MMP-7-IN-3 is added at concentrations ranging from 0.1-100 nM. The increase in fluorescence is measured (excitation 325 nm, emission 393 nm). The IC50 value is calculated from the dose-response curve.
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| Cell Assay |
For cell-based assays, cells that secrete MMP-7 (e.g., certain cancer cell lines or activated macrophages) are treated with MMP-7-IN-3 (0.1-10 uM). The conditioned media is collected after 24-48 hours, and the activity of MMP-7 in the media is measured using a FRET substrate. Cell viability is also assessed using an MTT or CellTiter-Glo assay to rule out cytotoxic effects. For fibrosis studies, activated fibroblasts or renal epithelial cells can be used.
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| Animal Protocol |
For animal studies, the unilateral ureteral obstruction (UUO) model is used in mice to induce renal fibrosis. MMP-7-IN-3 is administered intraperitoneally or orally to the mice, typically starting either at the time of surgery or shortly thereafter. Doses and dosing regimens (e.g., daily for 7-14 days) are optimized. At the end of the study, the kidneys are harvested, and the severity of fibrosis is assessed by histological methods (e.g., Masson's trichrome staining) and by measuring hydroxyproline content as a biochemical marker of collagen deposition. MMP-7 activity in kidney lysates is measured.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of MMP-7-IN-3 are not fully characterized in the available literature. It is typically dissolved in DMSO for in vitro studies. For in vivo use, the compound can be formulated in a vehicle such as a mixture of DMSO, PEG300, Tween-80, and saline. The compound is a solid and should be stored at -20degC, protected from light and moisture.
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| Toxicity/Toxicokinetics |
Detailed toxicological data for MMP-7-IN-3 are not available. In the UUO mouse model at the doses used to suppress fibrosis, the compound was likely well-tolerated as no overt signs of toxicity were reported. Standard safety precautions for handling research chemicals should be followed. As with any experimental compound, a full toxicological evaluation would be required before human use.
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| References | |
| Additional Infomation |
MMP-7-IN-3 is a powerful research tool for studying the role of MMP-7 in disease. Its potent activity (IC50 = 2.8 nM) and demonstrated in vivo efficacy in a renal fibrosis model make it a promising candidate for drug development. The compound has a molecular weight of 818.26 g/mol and a molecular formula of C34H43ClF3N7O9S. It is not an approved drug and is intended for research purposes only.
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| Exact Mass |
817.248
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| CAS # |
2865097-58-9
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| PubChem CID |
168719944
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
18
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| Heavy Atom Count |
55
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| Complexity |
1500
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CC(C)(C)[C@@H](C(=O)N1CCC[C@H]1CC(=O)N)NC(=O)[C@H](CC2=CC=NC=C2)NC(=O)CNC(=O)CC[C@@H](C(=O)O)NS(=O)(=O)C3=CC(=C(C=C3)Cl)C(F)(F)F
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| InChi Key |
ITXQTOBRXFVFDQ-OKEDDIKYSA-N
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| InChi Code |
InChI=1S/C34H43ClF3N7O9S/c1-33(2,3)29(31(50)45-14-4-5-20(45)16-26(39)46)43-30(49)25(15-19-10-12-40-13-11-19)42-28(48)18-41-27(47)9-8-24(32(51)52)44-55(53,54)21-6-7-23(35)22(17-21)34(36,37)38/h6-7,10-13,17,20,24-25,29,44H,4-5,8-9,14-16,18H2,1-3H3,(H2,39,46)(H,41,47)(H,42,48)(H,43,49)(H,51,52)/t20-,24-,25-,29+/m0/s1
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| Chemical Name |
(2S)-5-[[2-[[(2S)-1-[[(2S)-1-[(2S)-2-(2-amino-2-oxoethyl)pyrrolidin-1-yl]-3,3-dimethyl-1-oxobutan-2-yl]amino]-1-oxo-3-pyridin-4-ylpropan-2-yl]amino]-2-oxoethyl]amino]-2-[[4-chloro-3-(trifluoromethyl)phenyl]sulfonylamino]-5-oxopentanoic 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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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