| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 100mg |
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Purity: =99.62%
| Targets |
Mitochondrial cardiolipin
Elamipretide targets cardiolipin, a phospholipid found exclusively in the inner mitochondrial membrane. It specifically binds to cardiolipin through electrostatic and hydrophobic interactions, stabilizing the membrane curvature. This binding enhances mitochondrial membrane stability, reduces reactive oxygen species (ROS) production, and maintains electron transport chain supercomplex integrity. Elamipretide also acts as a cytochrome c peroxidase inhibitor. By targeting mitochondria, it prevents mitochondrial depolarization and reduces cell apoptosis. |
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| ln Vitro |
Barth syndrome is a rare X-linked genetic disorder characterized by mitochondrial dysfunction. Elamipretide is a mitochondrial cardiolipin binder that penetrates cells and accumulates in the mitochondria: It localizes to the inner mitochondrial membrane, improving mitochondrial morphology and function. Elamipretide's mechanism of action involves electrostatic interactions with cardiolipin, a phospholipid critical for mitochondrial structure and electron transport chain function. By binding to cardiolipin, elamipretide stabilizes the mitochondrial membrane, prevents oxidative damage, and maintains membrane potential. This interaction preserves cristae integrity, reduces reactive oxygen species (ROS) production, and maintains ATP production. Elamipretide also enhances the activity of mitochondrial respiratory complexes, facilitating efficient electron transfer and ATP synthesis. Furthermore, elamipretide inhibits the opening of the mitochondrial permeability transition pore (mPTP), protecting against mitochondrial damage during reperfusion and reducing cell death in ischemic conditions.
In vitro, Elamipretide reduces islet cell apoptosis, increases islet cell yield, and improves post-transplantation function. It prevents mitochondrial depolarization and scavenges reactive oxygen species, mitigating oxidative damage in neuronal cells and other cell types. The tetrapeptide improves mitochondrial dysfunction in cellular models and shows cytoprotective effects against oxidative stress-induced cell death. Its cardiolipin-binding activity stabilizes mitochondrial membranes and preserves ETC function. |
| ln Vivo |
Elamipretide is a mitochondrial cardiolipin binder that localizes to the inner mitochondrial membrane to improve mitochondrial morphology and function. Elamipretide was shown to attenuate neuronal oxidative stress and neuroinflammation, activate neural mitochondrial biogenesis, enhance mitochondrial respiration, and protect against neural apoptosis. Protective effects of elamipretide against neuronal loss and inflammation have been reported in traumatic brain injury, hind limb ischemia–reperfusion injury, type II diabetes, and spinal cord injury. Clinically significant QTc interval prolongation was not observed at three times the peak concentration of the maximum recommended dose.
Elamipretide is a mitochondrial cardiolipin binder being investigated for diseases involving mitochondrial dysfunction. Elamipretide is a synthetic tetrapeptide that selectively binds to cardiolipin, a phospholipid in the inner mitochondrial membrane. This interaction improves mitochondrial morphology and function. In September 2025, the U.S. Food and Drug Administration (FDA) granted accelerated approval for FORZINITY™ (elamipretide) to improve muscle strength in adult and pediatric patients with Barth syndrome weighing at least 30 kg. ELAMIPRETIDE is a Protein drug with a maximum clinical trial phase of III (across all indications) and has 10 investigational indications.
In vivo, Elamipretide improves left ventricular and mitochondrial function in dogs with advanced heart failure. It improves mitochondrial dysfunction, synaptic function, and memory impairment induced by lipopolysaccharide in mice. The compound mitigates oxidative damage by scavenging ROS and stabilizing cardiolipin, showing therapeutic potential in preclinical models of Barth syndrome and other mitochondrial disorders. It is also blood-brain-barrier permeable, enabling CNS applications. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for Elamipretide typically assess its binding to cardiolipin using surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC). Cytochrome c peroxidase activity can be measured spectrophotometrically by monitoring the oxidation of cytochrome c in the presence of hydrogen peroxide. ROS scavenging activity is assessed using cell-based or cell-free ROS detection assays (e.g., DCFH-DA). Mitochondrial membrane potential (ΔΨm) is measured using fluorescent dyes such as JC-1 or TMRM.
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| Cell Assay |
Cellular assays for Elamipretide utilize various cell types including neurons, cardiomyocytes, pancreatic islet cells, and astrocytes. Cells are treated with Elamipretide and then exposed to oxidative stress (e.g., H₂O₂, rotenone) or mitochondrial toxins. Readouts include cell viability (MTT), ROS levels (DCFH-DA), mitochondrial membrane potential (JC-1), ATP levels, and apoptosis markers (caspase-3/7, Annexin V). Islet cell yield and function are assessed in islet isolation models.
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| Animal Protocol |
In vivo animal studies for Elamipretide utilize models of heart failure, mitochondrial disease, neurodegeneration, and ischemia-reperfusion injury. The compound is administered via intraperitoneal, intravenous, or subcutaneous injection. Endpoints include cardiac function (echocardiography), mitochondrial function (respiratory chain enzyme activities), oxidative stress markers, behavioral assessments (memory, motor function), and histopathological analysis of tissue damage. Dosing is typically daily or twice daily.
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| ADME/Pharmacokinetics |
Absorption
After daily subcutaneous injection of 2 to 80 mg, ilapipritide exposure increases proportionally with increasing dose, with minimal accumulation. Maximum ilapipritide concentrations are reached 0.5 to 1 hour after subcutaneous injection. The absolute bioavailability after subcutaneous injection is approximately 92%. Exposure is comparable after subcutaneous injection into the thigh or abdomen. Elimination Route Ilamipretide and its metabolites M1 and M2 are excreted in the urine. In patients with normal renal function, approximately 100% of the ilapipritide dose is recovered in the urine 48 hours after administration, present as ilapipritide, M1, or M2. Volume of Distribution Ilamipretide is distributed in systemic water, with a volume of distribution of approximately 0.5 L/kg. Protein Binding Protein binding is approximately 39%. Metabolism/Metabolites Elamipretide is metabolized via C-terminal degradation into M1 tripeptide and M2 dipeptide metabolites, which are not pharmacologically active. Its metabolic pathway is not fully elucidated. Elamipretide is a tetrapeptide with molecular weight of approximately 640.8 g/mol. It is cell-permeable and has blood-brain-barrier permeability. Pharmacokinetic studies in preclinical species indicate that the compound has a short half-life requiring frequent dosing. It is administered via subcutaneous or intravenous injection. The peptide is metabolized by peptidases and excreted in urine. Its pharmacokinetic profile supports use in acute and chronic indications where mitochondrial protection is needed. |
| Toxicity/Toxicokinetics |
Preclinical toxicity studies indicate that Elamipretide is generally well-tolerated. In animal models, it has shown minimal toxicity and synergistic cell activity. The compound has been evaluated in clinical trials for mitochondrial diseases, heart failure, and Barth syndrome, with a favorable safety profile. Common adverse effects in clinical studies include injection site reactions (subcutaneous administration) and mild gastrointestinal symptoms. No significant organ toxicity has been reported at therapeutic doses.
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| References |
A mitochondrial therapeutic reverses visual decline in mouse models of diabetes. Dis Model Mech. 2015 Jul 1;8(7):701-10. doi: 10.1242/dmm.020248. Epub 2015 Apr 23. PubMed PMID: 26035391; PubMed Central PMCID: PMC4486862.
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| Additional Infomation |
Elamipretide has been used in trials investigating the treatment of Leber hereditary optic neuropathy.
Elamipretide (SS-31, MTP-131, Bendavia) is a mitochondria-targeting tetrapeptide antioxidant. It binds cardiolipin, stabilizes mitochondrial membranes, reduces ROS, and improves mitochondrial function. It has shown therapeutic potential in heart failure, Barth syndrome, and neurodegenerative diseases. Clinical trials have been conducted for mitochondrial myopathy and other indications. It is not yet FDA-approved but has been granted orphan drug status for Barth syndrome. |
| Molecular Formula |
C32H49N9O5
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|---|---|
| Molecular Weight |
639.7888
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| Exact Mass |
639.386
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| Elemental Analysis |
C, 60.07; H, 7.72; N, 19.70; O, 12.50
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| CAS # |
736992-21-5
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| Related CAS # |
736992-21-5;1334953-95-5 (acetate);2244098-12-0 (HCl);
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| PubChem CID |
11764719
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| Sequence |
H-D-Arg-Tyr(2,6-diMe)-Lys-Phe-NH2; D-arginyl-2,6-dimethyl-L-tyrosyl-L-lysyl-L-phenylalaninamide
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| SequenceShortening |
RXKF
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| Appearance |
White to off-white solid powder
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| LogP |
5.715
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| Hydrogen Bond Donor Count |
9
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
19
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| Heavy Atom Count |
46
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| Complexity |
991
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| Defined Atom Stereocenter Count |
4
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| SMILES |
O=C([C@]([H])(C([H])([H])C1C(C([H])([H])[H])=C([H])C(=C([H])C=1C([H])([H])[H])O[H])N([H])C([C@@]([H])(C([H])([H])C([H])([H])C([H])([H])/N=C(\N([H])[H])/N([H])[H])N([H])[H])=O)N([H])[C@]([H])(C(N([H])[C@]([H])(C(N([H])[H])=O)C([H])([H])C1C([H])=C([H])C([H])=C([H])C=1[H])=O)C([H])([H])C([H])([H])C([H])([H])C([H])([H])N([H])[H]
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| InChi Key |
SFVLTCAESLKEHH-WKAQUBQDSA-N
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| InChi Code |
InChI=1S/C32H49N9O5/c1-19-15-22(42)16-20(2)23(19)18-27(41-29(44)24(34)11-8-14-38-32(36)37)31(46)39-25(12-6-7-13-33)30(45)40-26(28(35)43)17-21-9-4-3-5-10-21/h3-5,9-10,15-16,24-27,42H,6-8,11-14,17-18,33-34H2,1-2H3,(H2,35,43)(H,39,46)(H,40,45)(H,41,44)(H4,36,37,38)/t24-,25+,26+,27+/m1/s1
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| Chemical Name |
(S)-6-amino-N-((S)-1-amino-1-oxo-3-phenylpropan-2-yl)-2-((S)-2-((R)-2-amino-5-guanidinopentanamido)-3-(4-hydroxy-2,6-dimethylphenyl)propanamido)hexanamide
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| Synonyms |
MTP 131; MTP-131; Elamipretide; 736992-21-5; bendavia; Ocuvia; MTP131; Bendavia; RX-31; Elamipretide; SS-31; D-Arg-Dmt-Lys-Phe-NH2.
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5630 mL | 7.8151 mL | 15.6301 mL | |
| 5 mM | 0.3126 mL | 1.5630 mL | 3.1260 mL | |
| 10 mM | 0.1563 mL | 0.7815 mL | 1.5630 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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