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首页 / 抑制剂/激动剂 / 代谢酶 / Cardiolipin Peroxidase / Elamipretide

Elamipretide {[allProObj[0].p_purity_real_show]}

货号：A350353 同义名： MTP-131; RX-31

Elamipretide是一种线粒体靶向肽，作为心磷脂过氧化物酶抑制剂，具有改善心肌梗死、肾功能、神经保护作用，减轻氧化应激和炎症损伤。

Elamipretide 化学结构 CAS号：736992-21-5
Elamipretide 化学结构
CAS号：736992-21-5
Elamipretide 3D分子结构
CAS号：736992-21-5
Elamipretide 化学结构 CAS号：736992-21-5
Elamipretide 3D分子结构 CAS号：736992-21-5
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Elamipretide 纯度/质量文件 产品仅供科研

货号：A350353 标准纯度： {[allProObj[0].p_purity_real_show]}
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Elamipretide 生物活性

描述 Impaired mitochondrial (MITO) energy metabolism plays a key pathogenic role in agerelated degenerative disorders and is centrally involved in organ ischemia/reperfusion injury. Abnormalities of MITO structure and function exist in the failing heart of humans and experimental animals evidenced by hyperplasia, reduced organelle size, diminished rate of ATP synthesis and increased formation of reactive oxygen species (ROS)[3]. Elamipretide (MTP-131), a novel mitochondria-targeting peptide, was shown to reduce infarct size in animals with myocardial infarction and improve renal function in pigs with acute and chronic kidney injury[3]. Long-term therapy with elamipretide improved left ventricular (LV) systolic function, normalized plasma biomarkers and reversed MITO abnormalities in LV myocardium of dogs with advanced heart failure (HF). The results supported the development of elamipretide for the treatment of HF[3]. Patients with heart failure with reduced ejection fraction (ejection fraction, ≤35%) are randomized to either a single 4-hour infusion of elamipretide (0.25 mg/kg/h) or placebo control. Compared with placebo, a significant decrease in left ventricular end-diastolic volume and end-systolic volume occured at end infusion in the highest dose cohort, which demonstrated that a single infusion of elamipretide was safe and well tolerated[4].

Elamipretide 动物研究

Dose Rat: 5 mg/kg[3] (i.p.)
Administration i.p.

Elamipretide 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02367014 Mitochondrial Myopathy Phase 1 Phase 2 Completed - United States, California ... 展开 >> University of California San Diego, California, United States United States, Massachusetts Massachusetts General Hospital Boston, Massachusetts, United States United States, Ohio Akron Children's Hospital Akron, Ohio, United States United States, Pennsylvania Children's Hospital of Pittsburg of UPMC Pittsburgh, Pennsylvania, United States 收起 <<
NCT02245620 Skeletal Muscle Mitochondrial ... 展开 >>Dysfunction in the Elderly 收起 << Phase 2 Completed - United States, Washington ... 展开 >> Seattle, Washington, United States 收起 <<
NCT01755858 Renal Artery Obstruction ... 展开 >> Hypertension, Renovascular Ischemia Reperfusion Injury 收起 << Phase 1 Phase 2 Terminated - United States, Minnesota ... 展开 >> Mayo Clinic Rochester, Minnesota, United States, 55905 收起 <<

Elamipretide 参考文献

[1]Saad A, Herrmann SMS, et al. Phase 2a Clinical Trial of Mitochondrial Protection (Elamipretide) During Stent Revascularization in Patients With Atherosclerotic Renal Artery Stenosis. Circ Cardiovasc Interv. 2017 Sep;10(9). pii: e005487.

[2]Sabbah HN, Gupta RC, et al. Chronic Therapy With Elamipretide (MTP-131), a Novel Mitochondria-Targeting Peptide, Improves Left Ventricular and Mitochondrial Function in Dogs With Advanced Heart Failure. Circ Heart Fail. 2016 Feb;9(2):e002206.

[3]Sabbah HN, Gupta RC, Kohli S, Wang M, Hachem S, Zhang K. Chronic Therapy With Elamipretide (MTP-131), a Novel Mitochondria-Targeting Peptide, Improves Left Ventricular and Mitochondrial Function in Dogs With Advanced Heart Failure. Circ Heart Fail. 2016 Feb;9(2):e002206. doi: 10.1161/CIRCHEARTFAILURE.115.002206. PMID: 26839394; PMCID: PMC4743543.

[4]Daubert MA, Yow E, Dunn G, Marchev S, Barnhart H, Douglas PS, O'Connor C, Goldstein S, Udelson JE, Sabbah HN. Novel Mitochondria-Targeting Peptide in Heart Failure Treatment: A Randomized, Placebo-Controlled Trial of Elamipretide. Circ Heart Fail. 2017 Dec;10(12):e004389. doi: 10.1161/CIRCHEARTFAILURE.117.004389. PMID: 29217757.

Elamipretide 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.56mL

0.31mL

0.16mL

7.82mL

1.56mL

0.78mL

15.63mL

3.13mL

1.56mL

Elamipretide 技术信息

CAS号736992-21-5
分子式C32H49N9O5
分子量 639.79
SMILES Code O=C(N)[C@H](CC1=CC=CC=C1)NC([C@H](CCCCN)NC([C@H](CC2=C(C)C=C(C=C2C)O)NC([C@@H](CCCNC(N)=N)N)=O)=O)=O
MDL No. MFCD20133791
别名 MTP-131; RX-31; D-Arg-Dmt-Lys-Phe-NH2; SS-31
运输蓝冰
InChI Key SFVLTCAESLKEHH-WKAQUBQDSA-N
Pubchem ID 11764719
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C
溶解方案

DMSO: 30 mg/mL(46.89 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

Tags: Elamipretide |Elamipretide | MTP-131 | RX-31 | D-Arg-Dmt-Lys-Phe-NH2 | SS-31 | 736992-21-5 | Cardiolipin Peroxidase | Elamipretide 纯度/质量文件 | Elamipretide 生物活性 | Elamipretide 动物研究 | Elamipretide 临床数据 | Elamipretide 参考文献 | Elamipretide 实验方案 | Elamipretide 技术信息

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