| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
Mitochondria (damaged organelles). Mitochondria degrader-1 targets damaged mitochondria and induces their degradation through the autophagy mechanism (mitophagy). By promoting the clearance of dysfunctional mitochondria, the compound maintains cellular homeostasis and may protect against diseases associated with mitochondrial dysfunction, including neurodegenerative and metabolic disorders.
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| ln Vitro |
Mitochondria degrader-1 induces the autophagic degradation of damaged mitochondria. In vitro studies demonstrate that the compound promotes mitophagy, leading to the clearance of dysfunctional mitochondria from cells. This activity is likely measured by assessing mitochondrial mass, membrane potential, and the colocalization of mitochondria with autophagic markers such as LC3. The specific potency is not detailed in reference sources.
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| ln Vivo |
No in vivo activity data for Mitochondria degrader-1 are provided in the reference sources. Based on its mechanism, in vivo studies would likely involve animal models of neurodegenerative disease (e.g., Parkinson's or Alzheimer's models), metabolic disorders, or age-related diseases, with the compound administered systemically to assess mitigation of disease phenotypes.
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| Enzyme Assay |
Not explicitly detailed in reference sources. A typical mitophagy assay involves treating cells with a mitochondrial uncoupler (e.g., CCCP) to induce mitochondrial damage, then adding Mitochondria degrader-1. Mitophagy is assessed by measuring colocalization of mitochondria with LC3 by immunofluorescence, detecting mitochondrial protein degradation by Western blot, or using a mitophagy reporter system (e.g., mt-Keima).
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| Cell Assay |
Cells (e.g., HeLa or neuronal cell lines) are treated with Mitochondria degrader-1 at various concentrations for 6-24 hours. Mitochondrial function is assessed by MTT assay or Seahorse metabolic analysis. Mitophagy is quantified by Western blot for mitochondrial proteins (e.g., TOM20, COXIV) or by flow cytometry using mitophagy-specific dyes.
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| Animal Protocol |
No animal experimental protocols for Mitochondria degrader-1 are provided in the reference sources. A typical in vivo study for a mitophagy inducer might use a mouse model of neurodegenerative disease (e.g., MPTP-induced Parkinson's model), administering the compound daily by oral gavage or intraperitoneal injection for 2-4 weeks, followed by assessment of mitochondrial function in brain tissue, motor behavior, and neuropathology.
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| ADME/Pharmacokinetics |
Mitochondria degrader-1 has a molecular weight of 758.30 and formula C33H49ClFN7O8S. It is soluble in DMSO (≥100 mg/mL, 131.87 mM). Storage should be at -20degC as powder; in solution at -80degC, it is stable for 6 months. For in vivo formulation, various co-solvent systems may be used (e.g., 10% DMSO + 40% PEG300 + 5% Tween80 + 45% saline).
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| Toxicity/Toxicokinetics |
No toxicity data for Mitochondria degrader-1 are provided in the reference sources. As a research tool for inducing mitophagy, comprehensive toxicity studies would be required for any potential therapeutic use. The compound is for research use only and should be handled with appropriate safety precautions.
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| References | |
| Additional Infomation |
Mitochondria degrader-1 (Example 5 in patent WO2019013181A1) is a research compound not yet approved for clinical use. It is a chemical tool for studying the role of damaged mitochondria in disease and for validating mitophagy as a therapeutic strategy. The compound may have applications across multiple disease areas where mitochondrial dysfunction plays a pathogenic role.
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| Molecular Formula |
C33H49CLFN7O8S
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|---|---|
| Molecular Weight |
758.30
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| Exact Mass |
757.303
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| CAS # |
2241669-05-4
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| PubChem CID |
142408984
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| Appearance |
Light yellow to yellow ointment
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| LogP |
1.4
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
28
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| Heavy Atom Count |
51
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| Complexity |
1050
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC(=O)N[C@@H](CSC1=NC2=C(N1CC3=CC=C(C=C3)F)N=C(NC2=O)N)C(=O)NCCOCCOCCOCCOCCOCCCCCCCl
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| InChi Key |
JIUOEUKVQTVYRY-MHZLTWQESA-N
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| InChi Code |
InChI=1S/C33H49ClFN7O8S/c1-24(43)38-27(23-51-33-39-28-29(40-32(36)41-31(28)45)42(33)22-25-6-8-26(35)9-7-25)30(44)37-11-13-47-15-17-49-19-21-50-20-18-48-16-14-46-12-5-3-2-4-10-34/h6-9,27H,2-5,10-23H2,1H3,(H,37,44)(H,38,43)(H3,36,40,41,45)/t27-/m0/s1
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| Chemical Name |
(2R)-2-acetamido-3-[[2-amino-9-[(4-fluorophenyl)methyl]-6-oxo-1H-purin-8-yl]sulfanyl]-N-[2-[2-[2-[2-[2-(6-chlorohexoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethyl]propanamide
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 (~131.87 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 | 1.3187 mL | 6.5937 mL | 13.1874 mL | |
| 5 mM | 0.2637 mL | 1.3187 mL | 2.6375 mL | |
| 10 mM | 0.1319 mL | 0.6594 mL | 1.3187 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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