Elamipretide - CAS 736992-21-5
Catalog number: B0084-476588
Category: Inhibitor
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Molecular Formula:
C32H49N9O5
Molecular Weight:
639.80
COA:
Inquire
Targets:
Others
Description:
Elamipretide is a cardiolipin peroxidase inhibitor and mitochondria-targeting peptide under the development of Stealth BioTherapeutics. It can Improve left Ventricular and Mitochondrial Function. Elamipretide can alleviate mitochondrial dysfunction and oxidative damage in human trabecular meshwork cells. It can prevent both iHTM and GTM(3) cells from sustained oxidative stress induced by H(2)O(2). Phase II clinical trials for the treatment of Chronic heart failure and Mitochondrial myopathies are ongoing.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-476588 10 mg $799 In stock
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Purity:
98%
Appearance:
Powder
Synonyms:
Bendavia; ELA 4; MTP 131; MTP131; MTP-131; Ocuvia; SBT-31; SPI-31; SS-31;(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
Solubility:
DMSO: ≥ 29 mg/mL
Storage:
-20℃ Freezer
MSDS:
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Application:
Chronic heart failure; Mitochondrial myopathies
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
InChIKey:
SFVLTCAESLKEHH-WKAQUBQDSA-N
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
Canonical SMILES:
Cc1cc(cc(c1C[C@@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N)NC(=O)[C@@H](CCCNC(=N)N)N)C)O
Current Developer:
Stealth BioTherapeutics
1.Rationale and design of the EMBRACE STEMI study: a phase 2a, randomized, double-blind, placebo-controlled trial to evaluate the safety, tolerability and efficacy of intravenous Bendavia on reperfusion injury in patients treated with standard therapy including primary percutaneous coronary intervention and stenting for ST-segment elevation myocardial infarction.
Chakrabarti AK;Feeney K;Abueg C;Brown DA;Czyz E;Tendera M;Janosi A;Giugliano RP;Kloner RA;Weaver WD;Bode C;Godlewski J;Merkely B;Gibson CM Am Heart J. 2013 Apr;165(4):509-514.e7. doi: 10.1016/j.ahj.2012.12.008. Epub 2013 Feb 15.
BACKGROUND: ;Although significant efforts have been made to improve ST-segment elevation myocardial infarction (STEMI) outcomes by reducing symptom-onset-to-reperfusion times, strategies to decrease the clinical impact of ischemic reperfusion injury have demonstrated limited success. Bendavia, an intravenously administered mitochondrial targeting peptide, has been shown to reduce myocardial infarct size and attenuate coronary no-reflow in experimental modelswhen given before reperfusion.;DESIGN: ;The EMBRACE STEMI study is a phase 2a, randomized, double-blind, placebo-controlled trial enrolling 300 patients with a first-time anterior STEMI and an occluded proximal or mid-left anterior descending artery undergoing primary percutaneous coronary intervention (PCI) within 4 hours of symptom onset. Patients will be randomized to receive either Bendavia at 0.05 mg/kg per hour or an identically appearing placebo administered as an intravenous infusion at 60 mL/h. The primary end point is infarct size measured by the area under the creatine kinase-MB enzyme curve calculated from measurements from the central clinical chemistry laboratory obtained over the initial 72 hours after the primary PCI procedure, and the major secondary end point is infarct size calculated by the volume of infarcted myocardium (late contrast gadolinium enhancement) on the day 4±1 cardiac magnetic resonance imaging.
2.Experimental coronary artery stenosis accelerates kidney damage in renovascular hypertensive swine.
Sun D;Eirin A;Zhu XY;Zhang X;Crane JA;Woollard JR;Lerman A;Lerman LO Kidney Int. 2015 Apr;87(4):719-27. doi: 10.1038/ki.2014.343. Epub 2014 Oct 22.
The impact of coronary artery stenosis (CAS) on renal injury is unknown. Here we tested whether the existence of CAS, regardless of concurrent atherosclerosis, would induce kidney injury and magnify its susceptibility to damage from coexisting hypertension (HT). Pigs (seven each) were assigned to sham, left-circumflex CAS, renovascular HT, and CAS plus HT groups. Cardiac and nonstenotic kidney functions, circulating and renal inflammatory and oxidative markers, and renal and microvascular remodeling were assessed 10 weeks later. Myocardial perfusion declined distal to CAS. Systemic levels of PGF2-α isoprostane, a marker of oxidative stress, increased in CAS and CAS plus HT, whereas single-kidney blood flow responses to acetylcholine were significantly blunted only in CAS plus HT compared with sham, HT, and CAS, indicating renovascular endothelial dysfunction. Tissue expression of inflammatory and oxidative markers were elevated in the CAS pig kidney, and further magnified in CAS plus HT, whereas angiogenic factor expression was decreased. Bendavia, a mitochondria-targeted peptide, decreased oxidative stress and improved renal function and structure in CAS. Furthermore, CAS and HT synergistically amplified glomerulosclerosis and renal fibrosis.
3.Novel Mitochondria-Targeting Peptide in Heart Failure Treatment: A Randomized, Placebo-Controlled Trial of Elamipretide.
Daubert MA;Yow E;Dunn G;Marchev S;Barnhart H;Douglas PS;O'Connor C;Goldstein S;Udelson JE;Sabbah HN Circ Heart Fail. 2017 Dec;10(12). pii: e004389. doi: 10.1161/CIRCHEARTFAILURE.117.004389.
BACKGROUND: ;Mitochondrial dysfunction and energy depletion in the failing heart are innovative therapeutic targets in heart failure management. Elamipretide is a novel tetrapeptide that increases mitochondrial energy; however, its safety, tolerability, and therapeutic effect on cardiac structure and function have not been studied in heart failure with reduced ejection fraction.;METHODS AND RESULTS: ;In this double-blind, placebo-controlled, ascending-dose trial, patients with heart failure with reduced ejection fraction (ejection fraction, ≤35%) were randomized to either a single 4-hour infusion of elamipretide (cohort 1 [n=8], 0.005; cohort 2 [n=8], 0.05; and cohort 3 [n=8], 0.25 mg·kg;-1;·h;-1;) or placebo control (n=12). Safety and efficacy were assessed by clinical, laboratory, and echocardiographic assessments performed at pre-, mid- and end-infusion and 6-, 8-, 12- and 24-hours postinfusion start. Peak plasma concentrations of elamipretide occurred at end-infusion and were undetectable by 24 hours postinfusion. There were no serious adverse events. Blood pressure and heart rate remained stable in all cohorts. Compared with placebo, a significant decrease in left ventricular end-diastolic volume (-18 mL; ;P;=0.
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CAS 736992-21-5 Elamipretide

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