| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
MuRF1-IN-1 targets muscle ring finger protein-1 (MuRF1), an E3 ubiquitin ligase that mediates the ubiquitination and degradation of structural proteins such as titin. By inhibiting MuRF1, the compound prevents the ubiquitin-proteasome-mediated breakdown of muscle proteins, preserving muscle mass and function in catabolic conditions. The primary mechanism of action is the targeted inhibition of MuRF1, a critical enzyme in the process of muscle protein degradation.
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| ln Vitro |
MuRF1-IN-1 effectively inhibits the interaction between MuRF1 and its substrate titin with an IC₅₀ value below 25 μM. It also inhibits E3 ligase activity of MuRF1. These in vitro activities demonstrate the compound's ability to disrupt MuRF1-mediated protein ubiquitination and degradation in muscle cells. The compound is a selective inhibitor of Muscle RING-Finger Protein-1.
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| ln Vivo |
MuRF1-IN-1 attenuates skeletal muscle atrophy and dysfunction in a mouse model of cardiac cachexia. Oral administration of the compound reduces muscle wasting and preserves contractile function, indicating its potential for treating muscle-wasting disorders associated with chronic diseases and aging. MuRF1-IN-1 (0.1% w/w; dietary administration; 7 weeks) has improvement effects in a mouse model of cardiac cachexia.
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| Enzyme Assay |
The inhibition of MuRF1-titin complexation can be assessed using biochemical binding or pull-down assays, where the compound's ability to disrupt the protein-protein interaction is measured. E3 ligase activity of MuRF1 can be evaluated using ubiquitination assays with recombinant MuRF1 and substrate proteins. The IC₅₀ for inhibition of MuRF1-titin complexation is below 25 μM.
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| Cell Assay |
MuRF1-IN-1 is evaluated in muscle cell lines to assess its effects on MuRF1-mediated protein degradation. Cells are treated with the compound, and the levels of MuRF1 substrates such as titin are measured by immunoblotting. The IC₅₀ for inhibition of MuRF1-titin complexation is determined.
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| Animal Protocol |
In vivo efficacy is evaluated in a mouse model of cardiac cachexia. Mice are administered MuRF1-IN-1 orally, and skeletal muscle atrophy and contractile dysfunction are assessed. Muscle mass, fiber cross-sectional area, and grip strength are measured to evaluate the compound's protective effects. MuRF1-IN-1 (0.1% w/w; dietary administration; 7 weeks) has improvement effects in a mouse model of cardiac cachexia.
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| ADME/Pharmacokinetics |
MuRF1-IN-1 is orally active. However, its pharmacokinetic limitations have been reported, leading to the development of optimized analogs such as MyoMed-205 and MyoMed-946 with improved serum stability. Detailed PK parameters have not been published. The compound is soluble in DMSO at 60 mg/mL.
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| Toxicity/Toxicokinetics |
No specific toxicity data have been reported for MuRF1-IN-1. As a research compound, it should be handled with standard laboratory safety precautions. Its safety profile in humans has not been evaluated. The compound is for research use only.
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| References | |
| Additional Infomation |
MuRF1-IN-1 is a research compound not approved for clinical use. It represents a first-in-class inhibitor identified from a screen against the MuRF1-titin interaction. The compound is a valuable tool for studying the role of MuRF1 in muscle wasting and for developing therapeutic strategies aimed at preserving muscle mass in cachexia, aging, and other catabolic conditions. It is a muscle ring finger 1 (MuRF1) inhibitor that attenuates skeletal muscle atrophy and dysfunction in cardiac cachexia.
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| Molecular Formula |
C18H15N3O3
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|---|---|
| Molecular Weight |
321.330003976822
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| Exact Mass |
321.111
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| CAS # |
445222-91-3
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| PubChem CID |
4661966
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
0.8
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
24
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| Complexity |
757
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN1C2=CC=CC=C2C3(C1=O)C(=C(OC4=C3C(=O)CCC4)N)C#N
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| InChi Key |
VXTHFLXWLSPJSP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H15N3O3/c1-21-12-6-3-2-5-10(12)18(17(21)23)11(9-19)16(20)24-14-8-4-7-13(22)15(14)18/h2-3,5-6H,4,7-8,20H2,1H3
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| Chemical Name |
2-amino-1'-methyl-2',5-dioxospiro[7,8-dihydro-6H-chromene-4,3'-indole]-3-carbonitrile
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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: 125 mg/mL (389.01 mM)
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1121 mL | 15.5603 mL | 31.1207 mL | |
| 5 mM | 0.6224 mL | 3.1121 mL | 6.2241 mL | |
| 10 mM | 0.3112 mL | 1.5560 mL | 3.1121 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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