| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Targets |
MASM-7 targets mitofusins (MFN1 and MFN2), which are key proteins involved in mitochondrial fusion. It directly activates MFN2 or MFN and can bind to the HR2 domain of MFN2. By activating mitofusins, MASM-7 promotes mitochondrial fusion, which is important for maintaining mitochondrial function, cellular metabolism, and quality control. Mitochondrial fusion defects are associated with various diseases including neurodegenerative disorders and metabolic diseases.
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| ln Vitro |
Through direct activation of MFN2 or MFN, MASM7 (1-10 μM, 2 h) enhances Mito AR in MEFs in a concentration-responsive manner (EC50 value: 75 nM). This can facilitate mitochondrial fusion [1]. Direct binding of MASM7 (1-1000 μM, 5 min) to the HR2 domain of MFN2 has been demonstrated, with a Kd value of 1.1 μM [1]. No cell lines experience DNA damage when exposed to 1 μM MASM7 for six hours [1]. MASM7 (0–1.5 μM, 6 h). Caspases 3/7 are not activated in U2OS cells by MASM7 (1 μM, 6 h) [1]. For a duration of 72 hours, MASM7 (0-1 μM, ) does not diminish cell viability [1]. In WT MEFs, it raises the potential of the mitochondrial membrane after 6 hours[1].
In vitro, MASM-7 increases Mito AR (a measure of mitochondrial fusion) with an EC50 of 75 nM in mouse embryonic fibroblasts (MEFs) in a concentration-responsive manner. It promotes mitochondrial fusion by directly activating MFN2 or MFN. The compound can directly bind to the HR2 domain of MFN2. These in vitro activities make MASM-7 a valuable tool for studying mitochondrial dynamics and the role of mitochondrial fusion in cellular physiology and disease. |
| ln Vivo |
In vivo studies with MASM-7 are limited. As a mitochondrial fusion activator, the compound has potential for studying mitochondrial dysfunction in vivo. However, specific in vivo efficacy data are not extensively documented. The compound is primarily used as a research tool for studying mitochondrial dynamics.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for MASM-7 involve studying its interaction with mitofusins. Binding to MFN2 can be assessed by surface plasmon resonance (SPR) or co-immunoprecipitation assays. The compound's ability to activate MFN2-mediated mitochondrial fusion can be assessed in cell-based fusion assays. These assays characterize the compound's mechanism of action as a mitofusin activator.
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| Cell Assay |
Cell-based assays for MASM-7 are conducted in mouse embryonic fibroblasts (MEFs) and other cell types. Cells are treated with the compound at various concentrations (EC50 = 75 nM). Mitochondrial fusion is assessed by measuring Mito AR (a mitochondrial morphology parameter) using fluorescence microscopy. Mitochondrial network morphology is evaluated by staining with mitochondrial dyes. These assays characterize the compound's ability to promote mitochondrial fusion.
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| Animal Protocol |
In vivo animal experiments with MASM-7 are not extensively documented. As a mitochondrial fusion activator, the compound could potentially be used in models of mitochondrial dysfunction, neurodegenerative diseases, or metabolic disorders. However, specific protocols are limited. Researchers should consult primary literature for updated information.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of MASM-7 have not been extensively characterized. The compound has molecular weight 453.58 and molecular formula C22H23N5O2S2. It is soluble in DMSO. Storage: appropriately. Specific PK parameters such as half-life, bioavailability, and tissue distribution have not been reported.
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| Toxicity/Toxicokinetics |
Safety and toxicology data for MASM-7 are limited. The compound is for research use only and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling the compound. The compound should be stored properly and disposed of in accordance with applicable regulations.
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| References | |
| Additional Infomation |
MASM-7 has CAS number 920868-45-7, molecular formula C22H23N5O2S2, and molecular weight 453.58. It is a mitofusin activator that achieves mitochondrial fusion via mitofusins. MASM7 increases Mito AR with EC50 = 75 nM in MEFs and promotes mitochondrial fusion by directly activating MFN2 or MFN. Purity: >99%. Not for human use; for research purposes only.
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| Molecular Formula |
C22H23N5O2S2
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|---|---|
| Molecular Weight |
453.580321550369
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| Exact Mass |
453.129
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| CAS # |
920868-45-7
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| PubChem CID |
16347380
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| Appearance |
Off-white to yellow solid powder
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| LogP |
3.9
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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 |
7
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| Heavy Atom Count |
31
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| Complexity |
687
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C12CCCC=1C(C(N)=O)=C(NC(=O)C(SC1N(C3=CC=CC=C3)C(C3CC3)=NN=1)C)S2
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| InChi Key |
MTAWXPCGCQTSOJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H23N5O2S2/c1-12(20(29)24-21-17(18(23)28)15-8-5-9-16(15)31-21)30-22-26-25-19(13-10-11-13)27(22)14-6-3-2-4-7-14/h2-4,6-7,12-13H,5,8-11H2,1H3,(H2,23,28)(H,24,29)
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| Chemical Name |
2-[2-[(5-cyclopropyl-4-phenyl-1,2,4-triazol-3-yl)sulfanyl]propanoylamino]-5,6-dihydro-4H-cyclopenta[b]thiophene-3-carboxamide
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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 : ~100 mg/mL (~220.47 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.51 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 25.0 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 (4.59 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 can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2047 mL | 11.0234 mL | 22.0468 mL | |
| 5 mM | 0.4409 mL | 2.2047 mL | 4.4094 mL | |
| 10 mM | 0.2205 mL | 1.1023 mL | 2.2047 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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