| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
Purity: =99.62%
| Targets |
Mitochondrial cardiolipin
The primary molecular target of Elamipretide Acetate is the mitochondrial inner membrane, specifically cardiolipin, a phospholipid that is abundant in the mitochondrial inner membrane. Elamipretide binds to cardiolipin with high affinity, localizing the peptide to the mitochondria. By binding to cardiolipin, Elamipretide stabilizes the mitochondrial inner membrane structure, protects the electron transport chain from oxidative damage, and reduces the production of mitochondrial reactive oxygen species (ROS). The peptide also scavenges free radicals directly, acting as an antioxidant. The compound's mechanism of action involves the preservation of mitochondrial function, reduction of oxidative stress, and protection against mitochondrial dysfunction. Elamipretide does not inhibit specific enzymes but rather acts through a membrane-stabilizing and antioxidant mechanism. This unique mechanism of action makes it a promising therapeutic for diseases characterized by mitochondrial dysfunction and oxidative stress. |
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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 activity of Elamipretide Acetate is characterized by its antioxidant and mitochondrial protective effects. In cell-based assays, Elamipretide reduces mitochondrial ROS production in various cell types, including neurons, cardiomyocytes, and fibroblasts. In SH-SY5Y neuroblastoma cells, Elamipretide reduces tert-butyl hydroperoxide-induced lipid peroxidation and apoptosis. The compound also protects cells from H₂O₂-induced oxidative damage. In cardiomyocytes, Elamipretide improves mitochondrial function, increases ATP production, and reduces cell death under stress conditions. In endothelial cells, the peptide protects against oxidative stress-induced dysfunction. The compound's antioxidant activity is typically measured using fluorescent probes for ROS (e.g., DCFH-DA, MitoSOX) and by assessing markers of lipid peroxidation (e.g., MDA, 4-HNE). Mitochondrial function is assessed by measuring oxygen consumption rate (OCR), ATP levels, and mitochondrial membrane potential (JC-1 or TMRE staining). The compound's EC50 for cytoprotection is typically in the low nanomolar to micromolar range. |
| 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 activity of Elamipretide Acetate has been demonstrated in various animal models of mitochondrial dysfunction and oxidative stress-related diseases. In models of heart failure, Elamipretide improves cardiac function, reduces infarct size, and decreases oxidative stress. In models of mitochondrial myopathy, the peptide improves mitochondrial function and exercise capacity. In models of neurodegenerative diseases, Elamipretide reduces oxidative stress, improves mitochondrial function, and protects against neuronal loss. The compound has also been studied in models of ischemia-reperfusion injury, acute kidney injury, and aging. In clinical studies, Elamipretide has been evaluated for the treatment of mitochondrial myopathy, heart failure, and other mitochondrial diseases. The compound's in vivo efficacy is attributed to its ability to target mitochondria, reduce oxidative stress, and preserve mitochondrial function. Dosing in animal studies typically ranges from 0.1 to 10 mg/kg administered subcutaneously or intravenously. |
| Enzyme Assay |
For in vitro mitochondrial function assays with Elamipretide Acetate, the following protocol is used: Cells (e.g., SH-SY5Y, H9c2 cardiomyocytes, or primary fibroblasts) are cultured in appropriate media at 37°C in 5% CO₂. Cells are seeded in 96-well or 24-well plates and allowed to adhere overnight. Elamipretide Acetate is dissolved in water or DMSO and diluted in culture medium to final concentrations ranging from 0.001 to 100 μM. Cells are pre-treated with the compound for 1-24 hours before exposure to oxidative stress (e.g., H₂O₂, tert-butyl hydroperoxide, or rotenone). Mitochondrial ROS production is measured using MitoSOX Red (5 μM, 30 minutes incubation, excitation 510 nm, emission 580 nm). Mitochondrial membrane potential is measured using JC-1 or TMRE staining. ATP levels are measured using a bioluminescence ATP assay kit. Oxygen consumption rate (OCR) is measured using a Seahorse extracellular flux analyzer. For assessment of lipid peroxidation, cells are lysed and MDA or 4-HNE levels are measured by ELISA or HPLC. Apoptosis is assessed by Annexin V-FITC/PI staining and flow cytometry.
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| Cell Assay |
For in vitro cell-based assays with Elamipretide Acetate, the following typical protocol is used: For neuroprotection studies, SH-SY5Y cells are differentiated with retinoic acid (10 μM) for 5-7 days. Differentiated neurons are treated with Elamipretide Acetate at concentrations of 0.01-10 μM for 2-24 hours, followed by exposure to oxidative stress (e.g., 100-500 μM H₂O₂ or 50-200 μM tert-butyl hydroperoxide) for 24 hours. Cell viability is assessed using the MTT or CellTiter-Glo assay. Neurite outgrowth is assessed by staining with anti-MAP2 antibody and measuring neurite length using ImageJ. For cardiomyocyte studies, H9c2 cells are treated with Elamipretide and exposed to hypoxia/reoxygenation or oxidative stress. Cell viability, mitochondrial function, and apoptosis are assessed. For endothelial cell studies, HUVECs are treated with Elamipretide and exposed to oxidative stress or inflammatory stimuli. Endothelial function is assessed by measuring NO production, tube formation, and cell migration.
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| Animal Protocol |
For in vivo animal studies with Elamipretide Acetate, the following general protocol is used: For heart failure models, male C57BL/6 mice (8-10 weeks old) are subjected to transverse aortic constriction (TAC) or myocardial infarction (MI) to induce heart failure. Elamipretide Acetate is administered subcutaneously or intraperitoneally at doses of 0.1, 0.3, 1, and 3 mg/kg daily for 2-4 weeks. Cardiac function is assessed by echocardiography (ejection fraction, fractional shortening). Infarct size is measured by triphenyltetrazolium chloride (TTC) staining. For mitochondrial myopathy models, mice with mitochondrial dysfunction are treated with Elamipretide and exercise capacity is assessed by treadmill testing. For pharmacokinetic studies, blood and tissue samples (heart, skeletal muscle, brain) are collected at various time points after dosing, and compound concentrations are analyzed by LC-MS/MS. For toxicology studies, animals are treated with the compound for up to 28 days, and clinical chemistry, hematology, and histopathology are assessed.
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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. The pharmacokinetic properties of Elamipretide Acetate have been characterized in preclinical and clinical studies. After subcutaneous administration, Elamipretide is rapidly absorbed with peak plasma concentrations reached within 0.5-2 hours (Tmax). The compound has a small volume of distribution (approximately 0.2-0.5 L/kg), consistent with its distribution primarily in the extracellular space. However, the compound is taken up by mitochondria in tissues, resulting in high tissue-to-plasma ratios. Plasma protein binding is low to moderate. The elimination half-life is approximately 2-4 hours in humans, requiring once or twice daily dosing. Elamipretide is metabolized by peptidases to amino acids, which are recycled or excreted. The compound is primarily eliminated in urine. The compound's pharmacokinetics are linear over the therapeutic dose range. Elamipretide has been shown to accumulate in mitochondria, where it exerts its pharmacological effects. The compound's favorable pharmacokinetic profile supports its use in clinical trials for mitochondrial diseases. |
| Toxicity/Toxicokinetics |
The toxicity profile of Elamipretide Acetate is favorable based on preclinical and clinical studies. The compound has a wide therapeutic index with low toxicity. In preclinical studies, Elamipretide has not shown significant toxicity at doses up to 10-30 mg/kg/day in rodents and dogs. In clinical trials, the most common adverse effects are mild and include injection site reactions (for subcutaneous administration), headache, and gastrointestinal disturbances. Serious adverse effects are rare. The compound is not mutagenic or genotoxic in standard assays. Elamipretide is not carcinogenic in long-term studies. The compound's safety profile is consistent with its mechanism of action as a mitochondrial-targeted antioxidant. Elamipretide is not recommended during pregnancy and lactation unless the potential benefit justifies the potential risk to the fetus or infant. The compound's favorable safety profile supports its continued development for mitochondrial diseases.
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| References |
[1]. https://pubchem.ncbi.nlm.nih.gov/compound/11764719
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| Additional Infomation |
Elamipretide is a mitochondrial cardiolipin binder currently under investigation for its efficacy in treating diseases related to mitochondrial dysfunction. Ilamipreptide is a synthetic tetrapeptide that selectively binds to cardiolipin, a phospholipid on the inner mitochondrial membrane. This interaction can improve mitochondrial morphology and function. In September 2025, the U.S. Food and Drug Administration (FDA) granted accelerated approval to FORZINITY™ (imlamipreptide) for improving muscle strength in adults and children with Barth syndrome weighing at least 30 kg. Ilamipreptide is a protein-based drug that has completed up to three Phase III clinical trials (covering all indications) and has 10 investigational indications.
Elamipretide Acetate (CAS# 1334953-95-5) is a mitochondria-targeting peptide (MTP-131, SS-31) with potent antioxidant activity. It has a molecular formula of C34H53N9O5 and a molecular weight of approximately 699.84 g/mol. It reduces mitochondrial ROS and scavenges free radicals. Future research could focus on expanding its clinical applications to other mitochondrial diseases, developing oral formulations for improved patient convenience, and investigating its potential in neurodegenerative and age-related diseases. |
| Molecular Formula |
C34H53N9O7
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|---|---|
| Molecular Weight |
699.84
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| Exact Mass |
699.406
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| CAS # |
1334953-95-5
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| Related CAS # |
736992-21-5;1334953-95-5 (acetate);2244098-12-0 (HCl); 1606994-55-1
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| PubChem CID |
163336973
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| Sequence |
H-D-Arg-Tyr(2,6-diMe)-Lys-Phe-NH2.CH3CO2H; D-arginyl-2,6-dimethyl-L-tyrosyl-L-lysyl-L-phenylalaninamide acetic acid
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| SequenceShortening |
RXKF
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| Appearance |
Solid powder
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| Hydrogen Bond Donor Count |
10
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
19
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| Heavy Atom Count |
50
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| Complexity |
1020
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CC1=CC(=CC(=C1C[C@@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC2=CC=CC=C2)C(=O)N)NC(=O)[C@@H](CCCN=C(N)N)N)C)O.CC(=O)O
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| InChi Key |
UEYRJRBULBAAEG-NFWUDPOKSA-N
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| InChi Code |
InChI=1S/C32H49N9O5.C2H4O2/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;1-2(3)4/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);1H3,(H,3,4)/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 acetate
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| Synonyms |
SS31; MTP 131 acetate; SS-31; MTP131 acetate; Elamipretide Acetate; 1334953-95-5; MTP 131 acetate; acetic acid;(2S)-6-amino-2-[[(2S)-2-[[(2R)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]hexanamide; MTP 131 (acetate);SS 31; MTP-131 acetate
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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 | 1.4289 mL | 7.1445 mL | 14.2890 mL | |
| 5 mM | 0.2858 mL | 1.4289 mL | 2.8578 mL | |
| 10 mM | 0.1429 mL | 0.7144 mL | 1.4289 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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