Description | Elamipretide (MTP-131) is a mitochondria-targeted antioxidant tetrapeptide (D-Arg-dimethylTyr-Lys-Phe-NH2) that reduces toxic reactive oxygen species (ROS) production and stabilizes cardiolipin, with blood-brain-barrier permeability. Elamipretide is a potential therapeutic agent in the rare disease of Barnes syndrome. |
In vitro | 方法:大鼠胰岛素瘤细胞 INS1 用 Elamipretide (1-10 μM) 处理 20 h,使用 Immunofluorescence 检测细胞线粒体。结果:Elamipretide 可防止营养过剩引起的线粒体断裂,同时对健康 INS1 细胞的线粒体形态没有影响。[1]方法:永生化人小梁网细胞 iHTM 和青光眼人小梁细胞系 GTM3 细胞用 Elamipretide (0.01-1 μM) 预处理 1 h,随后用 H2O2 (200 μM) 孵育 24 h,使用 calorimetric assay 检测 LDH 释放。结果:H2O2 孵育导致 iHTM 和 GTM3 细胞中 LDH 释放显著增加,用 MTP-131 预处理可剂量依赖性抑制 LDH 释放。[2] |
In vivo | 方法:为研究对炎症和氧化应激的认知后遗症的影响,将 Elamipretide (5 mg/kg) 腹腔注射给注射 LPS 的 C57BL/6 小鼠,每天一次,持续三天。结果:LPS 诱导的记忆损伤可以通过线粒体靶向抗氧化剂 Elamipretide 来减轻。[3]方法:为检测对小鼠衰老的表型影响,将 Elamipretide (3 mg/kg) 皮下注射给 C57BL/6 小鼠,每周五次,持续十个月。结果:Elamipretide 增强了雄性和雌性小鼠的健康衰老和心脏功能,尽管对功能的具体影响因性别而异。在女性中,这种治疗可以提高认知能力和维持身体成分,而在男性中,旋转棒的表现得以保留。[4] |
Synonyms | MTP-131, RX-31, SS-31 |
molecular weight | 639.79 |
Molecular formula | C32H49N9O5 |
CAS | 736992-21-5 |
Storage | store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility | H2O: 100 mg/mL (156.30 mM) 5% DMSO+95% Saline: 1.45 mg/mL (2.27 mM) DMSO: 29 mg/mL (45.33 mM) |
References | 1. Petcherski A, et al. Elamipretide Promotes Mitophagosome Formation and Prevents Its Reduction Induced by Nutrient Excess in INS1 β-cells. J Mol Biol. 2018 Dec 7;430(24):4823-4833. 2. Chen M, et al. Mitochondria-targeted peptide MTP-131 alleviates mitochondrial dysfunction and oxidative damage in human trabecular meshwork cells. Invest Ophthalmol Vis Sci. 2011 Sep 1;52(10):7027-37. 3. Zhao W, et al. Elamipretide (SS-31) improves mitochondrial dysfunction, synaptic and memory impairment induced by lipopolysaccharide in mice. J Neuroinflammation. 2019 Nov 20;16(1):230. 4. Nickel K, et al. Long-term treatment with Elamipretide enhances healthy aging phenotypes in mice. Aging Pathobiol Ther. 2022;4(3):76-83. |
Citations | 1. Suo M, Qi Y, Liu L, et al. SS31 Alleviates Pressure Overload-Induced Heart Failure Caused by Sirt3-Mediated Mitochondrial Fusion. Frontiers in Cardiovascular Medicine. 2022.9 2. Yao S, Wu D, Hu X, et al.Platelet Membrane-Coated Bio-Nanoparticles of Indocyanine Green/Elamipretide for NIR Diagnosis and Antioxidant Therapy in Acute Kidney Injury.Acta Biomaterialia.2023 3. Hao Y, Fan Y, Feng J, et al.ALCAT1-mediated abnormal cardiolipin remodelling promotes mitochondrial injury in podocytes in diabetic kidney disease.Cell Communication and Signaling.2024, 22(1): 1-20. 4. Ji Y, Ma Y, Ma Y, et al.SS-31 inhibits mtDNA–cGAS–STING signaling to improve POCD by activating mitophagy in aged mice.Inflammation Research.2024: 1-14. |