Elamipretide (MTP-131)

For research use only.

Catalog No.S9803 Synonyms: SS-31, D-Arg-Dmt-Lys-Phe-NH2

Elamipretide (MTP-131) Chemical Structure

CAS No. 736992-21-5

Elamipretide (MTP-131, SS-31, D-Arg-Dmt-Lys-Phe-NH2) is a cytochrome c peroxidase inhibitor. Elamipretide improves mitochondrial dysfunction, synaptic and memory impairment induced by lipopolysaccharide in mice.

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Biological Activity

Description Elamipretide (MTP-131, SS-31, D-Arg-Dmt-Lys-Phe-NH2) is a cytochrome c peroxidase inhibitor. Elamipretide improves mitochondrial dysfunction, synaptic and memory impairment induced by lipopolysaccharide in mice.
Targets
cytochrome c peroxidase [1]
()
In vitro

SS-31 binds with high affinity to cardiolipin, an anionic phospholipid expressed on the inner mitochondrial membrane that is required for cristae formation. In addition, the SS-31/cardiolipin complex inhibits cytochrome c peroxidase activity, which catalyzes cardiolipin peroxidation and results in mitochondrial damage during ischemia, by protecting its heme iron.[1]

In vivo

Pretreatment of rats with SS-31 protects cristae membranes during renal ischemia and prevents mitochondrial swelling. Prompt recovery of ATP on reperfusion leads to rapid repair of ATP-dependent processes, such as restoration of the actin cytoskeleton and cell polarity. Rapid recovery of ATP also inhibits apoptosis, protects tubular barrier function, and mitigates renal dysfunction.[1]

Protocol

Cell Research:

[1]

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  • Cell lines: feline kidney cells
  • Concentrations: 0.1-10 μM
  • Incubation Time: 1 hour
  • Method:

    Intracellular targeting of SS-31 is determined by incubating feline kidney cells, grown in biotin-free media for 24 hours, with biotinylated SS-31 for 1 hour. Cells are then fixed with 4% paraformaldehyde, permeabilized with 0.1% triton, and treated with Streptavidin-AlexaFluor594 for 30 minutes at room temperature. Fluorescence staining is observed by wide-field fluorescent microscope.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: male Sprague–Dawley rats
  • Dosages: 2.0 mg/kg
  • Administration: SC
    (Only for Reference)

Solubility (25°C)

In vitro Water 100 mg/mL (156.3 mM)
Ethanol '''-1 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 639.79
Formula

C32H49N9O5

CAS No. 736992-21-5
Storage powder
in solvent
Synonyms SS-31, D-Arg-Dmt-Lys-Phe-NH2

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02914665 Completed Drug: elamipretide|Drug: Placebo Heart Failure Stealth BioTherapeutics Inc. October 20 2016 Phase 2
NCT02848313 Completed Drug: Elamipretide Age-Related Macular Degeneration Stealth BioTherapeutics Inc. October 28 2016 Phase 1
NCT02814097 Completed Drug: elamipretide|Drug: Placebo Chronic Heart Failure Stealth BioTherapeutics Inc.|Charite University Berlin Germany|SCIRENT Clinical Research and Science d.o.o. September 2 2016 Phase 2
NCT02436447 Completed Drug: MTP-131 Normal and Impaired Renal Function Stealth BioTherapeutics Inc. May 2015 Phase 1
NCT02388529 Withdrawn Drug: MTP-131|Drug: Placebo Heart Failure Stealth BioTherapeutics Inc. May 2015 Phase 1

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID