SS-31肽是一种心磷脂过氧化物酶抑制剂和线粒体靶向肽。它可以改善左心室和线粒体功能。SS-31肽可减轻人小梁网状细胞中的线粒体功能障碍和氧化损伤。它可以防止iHTM和GTM（3）细胞受到H2O2诱导的持续氧化应激。治疗慢性心力衰竭和线粒体肌病的II期临床试验正在进行中。
编号：144820
CAS号：736992-21-5/1606994-55-1/1849610-71-4
单字母：H2N-r-Dmt-KF-CONH2
| 编号: | 144820 |
| 中文名称: | 线粒体靶向抗氧化剂SS-31：DArg-Dmt-Lys-Phe-NH2/依拉瑞肽/MTP-131 |
| 英文名: | Elamipretide |
| 英文同义词: | MTP-131 |
| CAS号: | 736992-21-5，醋酸体盐 1606994-55-1，TFA盐 1849610-71-4，3醋酸分子 |
| 单字母: | H2N-r-Dmt-KF-CONH2 |
| 三字母: | H2N N端氨基 -DArgD型精氨酸 -Dmt2,6-二甲基酪氨酸 -Lys赖氨酸 -Phe苯丙氨酸 -CONH2C端酰胺化 |
| 氨基酸个数: | 4 |
| 分子式: | C32H49N9O5 |
| 平均分子量: | 639.79 |
| 精确分子量: | 639.39 |
| 等电点(PI): | - |
| pH=7.0时的净电荷数: | 2.97 |
| 平均亲水性: | 1.1666666666667 |
| 疏水性值: | -1.87 |
| 外观与性状: | 白色粉末状固体 |
| 消光系数: | - |
| 来源: | 人工化学合成，仅限科学研究使用，不得用于人体。 |
| 纯度: | 98% |
| 生成周期: | 现货 |
| 储存条件: | 负80℃至负20℃ |
| 标签: | 氨基酸衍生物肽 D型氨基酸肽 |
| InChI: | (2R)-5-amino-2-[[2-[[(2S)-6-amino-2-[[(2R)-4-amino-2-[[(2R)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-amino-3-phenylpropanoyl]amino]-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]-3-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]-4-carboxybutanoyl]amino]-4-methylpentanoyl]amino]-5-oxopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-5-oxopentanoyl]amino]-4-carboxybutanoyl]amino]hexanoyl]amino]-4-carboxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-oxobutanoyl]amino]hexanoyl]amino]acetyl]amino]-5-oxopentanoic acid |
| IUPAC Name: | H-Phe-Val-Pro-Ile-Phe-Thr-Tyr-Gly-Glu-Leu-Gln-Arg-Leu-Gln-Glu-Lys-Glu-Arg-Asn-Lys-Gly-Gln-OH; L-phenylalanyl-L-valyl-L-prolyl-L-isoleucyl-L-phenylalanyl-L-threonyl-L-tyrosyl-glycyl-L-alpha-glutamyl-L-leucyl-L-glutaminyl-L-arginyl-L-leucyl-L-glutaminyl-L-alpha-glutamyl-L-lysyl-L-alpha-glutamyl-D-arginyl-D-asparagyl-L-lysyl-glycyl-D-glutamine; Motilin (swine), 13-L-leucine- |
SS-31肽是一种心磷脂过氧化物酶抑制剂和线粒体靶向肽。它可以改善左心室和线粒体功能。SS-31肽可减轻人小梁网状细胞中的线粒体功能障碍和氧化损伤。它可以防止iHTM和GTM（3）细胞受到H2O2诱导的持续氧化应激。治疗慢性心力衰竭和线粒体肌病的II期临床试验正在进行中。
H-Dmt-D-Arg-Phe-Lys-NH2 (Dmt:2,6-dimethyl-L-tyrosine) 是衍生与皮啡肽的阿片肽,它具有很强的镇痛作用和良好的细胞膜通过能力,在对其进行深入的机制研究后发现了线粒体靶向抗氧化肽SS-31 (H-D-Arg-Dmt-Lys-Phe-NH2). SS-31对缺血再灌注损伤、神经退行性疾病、心力衰竭、肌肉老化等和自由基有关的疾病具有治疗效果。SS-31 是一种针对线粒体的分子。它与心磷脂相互作用以重新激活缺血线粒体。同时SS-31也是一种细胞穿膜肽。
依拉瑞肽(MTP-131；D-Arg-DMT-Lys-Phe-NH2；其中DMT是2,6-二甲基-L-Tyr)是具有治疗缺血-再灌注损伤(例如，心脏缺血-再灌注损伤)和心肌梗塞的治疗潜力的线粒体靶向化合物。这种化合物的类似物可具有改善的治疗特征谱，包括改善的代谢性质、选择性或效力。
Elamipretide是一条由四个氨基酸组成的小分子多肽，在生物体内Elamipretide以线粒体内膜为靶点，能够预防神经细胞和其他细胞类型的氧化损伤；防止线粒体去极化，减少胰岛细胞凋亡，增加胰岛细胞产量，改善移植后功能。以Elamipretide为主要原料的药物已经进入临床三期。
Elamidetide is a small peptide composed of four amino acids, including one unnatural amino acid. In vivo, elamipretide can prevent oxidative damage of nerve cells and other cell types by targeting mitochondrial inner membrane, prevent mitochondrial depolarization, reduce apoptosis of islet cells, increase islet cell production, and improve the function after transplantation. The drugs with elamipretide as the main raw material have entered the third phase of clinical practice.
Elamipretide triacetate是一种芳香阳离子四肽，靶向线粒体内膜，是心磷脂过氧化物酶的抑制剂。它很容易穿透细胞膜，并已用于研究Leber遗传性视神经病变的治疗试验。
Elamipretide triacetate is an aromatic-cationic tetrapeptide that targets the mitochondrial intima and is an inhibitor of cardiolipin peroxidase. It easily penetrates cell membranes and has been used in therapeutic trials investigating Leber's Hereditary Optic Neuropathy.
很多蛋白在细胞中非常容易被降解，或被标记，进而被选择性地破坏。但含有部分D型氨基酸的多肽则显示了很强的抵抗蛋白酶降解能力。
| DOI | 名称 | |
|---|---|---|
| 10.1111/cbdd.12003 | Superior Analgesic Effect of H-Dmt-D-Arg-Phe-Lys-NH2 ([Dmt1]DALDA), a Multifunctional Opioid Peptide, Compared to Morphine in a Rat Model of Neuropathic Pain | 下载 |
| 10.1111_1440-1681.13484 | SS-31 protect retinal pigment epithelial cells from H2O2- induced cell injury by reducing apoptosis | 下载 |
| 10.1111_acel.13213 | SS-31 and NMN: Two paths to improve metabolism and function in aged hearts | 下载 |
| 10.1111_acel.12731 | Treatment with the mitochondrial-targeted antioxidant peptide SS-31 rescues neurovascular coupling responses and cerebrovascular endothelial function and improves cognition in aged mice | 下载 |
| 10.1111_bph.12468 | Targeting mitochondrial cardiolipin and the cytochrome c/cardiolipin complex to promote electron transport and optimize mitochondrial ATP synthesis | 下载 |
| 10.1155/2022/1295509 | SS-31, a Mitochondria-Targeting Peptide, Ameliorates Kidney Disease | 下载 |
| 10.1161/CIRCHEARTFAILURE.115.002206 | Chronic Therapy With Elamipretide (MTP-131), a Novel Mitochondria-Targeting Peptide, Improves Left Ventricular and Mitochondrial Function in Dogs With Advanced Heart Failure | 下载 |
| 编号 | 名称 | CAS号 |
| 432781 | Cys-SS-31 | |
| H2N-Cr-Dmt-KF-CONH2 | ||
| SS-31的N端添加半胱氨酸，引入巯基 | ||
