Elabela(19-32) TFA是一种与apelin受体（APJ）结合的内源性激动剂，能够激活Gαi1（EC50=8.6nM）和β-arrestin-2（EC50=166nM）信号通路
Sample solution is provided at 25 µL, 10mM.
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Elabela(19-32) TFA is an endogenous agonist that binds to the apelin receptor (APJ) and activates the Gαi1 (EC50=8.6nM) and β-arrestin-2 (EC50=166nM) signaling pathways[1-2]. Elabela(19-32) TFA is primarily used to study the pathophysiological mechanisms of cardiovascular diseases such as hypertension and heart failure, and is a potential therapeutic agent for cardiovascular diseases[3-4].
In vitro, pretreatment of H9c2 cardiomyocytes with Elabela(19-32) TFA (5nM), followed by hypoxia/reoxygenation (H/R) treatment to simulate myocardial ischemia-reperfusion injury. Elabela(19-32) TFA significantly inhibits apoptosis, reduces the expression of fibrosis markers (type I/III collagen), and improves mitochondrial dysfunction[5]. Treatment of HUVECs and EA.hy926 cells with Elabela(19-32) TFA (0.01–5μmol/L) for 6 or 24 hours. Elabela(19-32) TFA significantly enhances cell viability, promotes cell migration, and increases tube formation capacity[6].
In vivo, intraperitoneal injection of Elabela(19-32) TFA (0.5mg/kg/day) for 28 days in endothelial-specific ELA knockout mice and wild-type mice with hindlimb ischemia (HLI) models. Elabela(19-32) TFA markedly improves post-ischemic perfusion recovery and capillary density in ELA knockout mice, while upregulating the expression of VEGFR2, p-VEGFR2, and p-AKT[7]. In C57BL/6 mice with acute doxorubicin (15mg/kg, single intraperitoneal injection)-induced cardiotoxicity, subcutaneous administration of Elabela(19-32) TFA (2mg/kg) twice daily for 5 days. Elabela(19-32) TFA significantly improves cardiac function (left ventricular ejection fraction and fractional shortening), reduces serum levels of cardiac troponin T and creatine kinase-MB isoenzyme, and attenuates the decline in heart weight/body weight ratio and cardiomyocyte atrophy[8].
References:
[1] Sharma M, Prabhavalkar KS, Bhatt LK. Elabela Peptide: An Emerging Target in Therapeutics. Curr Drug Targets. 2022;23(14):1304-1318.
[2] Eberlé D, Marousez L, Hanssens S, et al. Elabela and Apelin actions in healthy and pathological pregnancies. Cytokine Growth Factor Rev. 2019 Apr;46:45-53.
[3] Gao S, Chen H. Therapeutic potential of apelin and Elabela in cardiovascular disease. Biomed Pharmacother. 2023 Oct;166:115268.
[4] Xu C. Cardiovascular aspects of ELABELA: A potential diagnostic biomarker and therapeutic target. Vascul Pharmacol. 2023 Aug;151:107193.
[5] Yu P, Ma S, Dai X, et al. Elabela alleviates myocardial ischemia reperfusion-induced apoptosis, fibrosis and mitochondrial dysfunction through PI3K/AKT signaling. Am J Transl Res. 2020 Aug 15;12(8):4467-4477.
[6] Wang X, Liang G, Guo Q, et al. ELABELA improves endothelial cell function via the ELA-APJ axis by activating the PI3K/Akt signalling pathway in HUVECs and EA.hy926 cells. Clin Exp Pharmacol Physiol. 2020 Dec;47(12):1953-1964.
[7] Peng JY, Fu X, Luo XY, et al. Endothelial ELABELA improves post-ischemic angiogenesis by upregulating VEGFR2 expression. Transl Res. 2024 Aug;270:13-23.
[8] Chen D, Yu W, Zhong C, et al. Elabela ameliorates doxorubicin-induced cardiotoxicity by promoting autophagic flux through TFEB pathway. Pharmacol Res. 2022 Apr;178:106186.
Elabela(19-32) TFA是一种与apelin受体（APJ）结合的内源性激动剂，能够激活Gαi1（EC50=8.6nM）和β-arrestin-2（EC50=166nM）信号通路[1-2]。Elabela(19-32) TFA多用于研究高血压、心力衰竭等心血管疾病的病理生理的机制，是潜在的心血管疾病治疗药物[3-4]。
在体外，Elabela(19-32) TFA（5nM）预处理H9c2心肌细胞，随后以缺氧/复氧（H/R）处理模拟心肌缺血再灌注损伤。Elabela(19-32) TFA显著抑制细胞凋亡、减轻纤维化标志物（I/III型胶原）表达、改善线粒体功能障碍[5]。Elabela(19-32) TFA（0.01–5μmol/L）处理HUVECs和EA.hy926细胞6或24小时，Elabela(19-32) TFA显著增强细胞活力、促进细胞迁移并提高管形成能力[6]。
在体内，Elabela(19-32) TFA（0.5mg/kg/day）腹腔注射28天，用于处理后肢缺血（HLI）模型的内皮特异性ELA敲除小鼠和野生型小鼠，显著改善了ELA敲除小鼠的缺血后灌注恢复和毛细血管密度，并上调了VEGFR2、p-VEGFR2和p-AKT的表达[7]。Elabela(19-32) TFA（2mg/kg）每日两次皮下注射，用于处理单次腹腔注射多柔比星（15mg/kg）诱导的急性心脏毒性C57BL小鼠模型，持续5天。Elabela(19-32) TFA显著改善了心脏功能（左心室射血分数和短轴缩短率），降低了血清心肌肌钙蛋白T和肌酸激酶同工酶水平，减轻了心脏重量/体重比值的下降和心肌细胞萎缩[8]。
| Cell experiment [1]: | |
Cell lines | H9c2 cells (rat ventricular cardiomyocyte cell line) |
Preparation Method | H9c2 cells were maintained in Dulbecco's minimal essential medium (DMEM) supplemented with 10% fetal bovine serum (FBS) at 37°C, 5% CO₂. H9c2 cells were treated with Hypoxia/Reoxygenation (H/R) to mimic myocardial ischemia/reperfusion injury in vitro, and then treated with Elabela(19-32) TFA (5nM) alone or in combination with LY294002 (10μM). |
Reaction Conditions | 5nM; treatment during H/R process |
Applications | Elabela(19-32) TFA significantly reduced H/R-induced apoptosis in H9c2 cells, as evidenced by decreased cleaved-caspase-3 and Bax expression, and increased Bcl-2 level. Elabela(19-32) TFA also ameliorated mitochondrial dysfunction by reducing reactive oxygen species (ROS) and malondialdehyde (MDA) production, while enhancing superoxide dismutase (SOD), glutathione (GSH) and ATP levels. These protective effects were mediated through activation of PI3K/AKT signaling pathway. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice |
Preparation Method | Mice were intraperitoneally administered a single dose of doxorubicin hydrochloride (DOX) (15mg/kg) to establish acute doxorubicin-induced cardiotoxicity (DIC) models. Elabela (19-32) TFA was administered subcutaneously (2mg/kg, twice daily) starting from the day of DOX injection. Mice were sacrificed on day 5 for analysis. |
Dosage form | 2mg/kg; i.p.; twice daily for 5 days. |
Applications | Elabela (19-32) TFA administration significantly ameliorated DOX-induced cardiac dysfunction, as evidenced by improved left ventricular ejection fraction (LVEF) and left ventricular fractional shortening (LVFS). Elabela (19-32) TFA treatment reduced myocardial injury, indicated by decreased serum levels of cardiac troponin T (cTnT) and creatine kinase-MB isoenzyme (CK-MB). Elabela (19-32) TFA alleviated DOX-induced cardiac atrophy, as shown by increased heart weight/body weight (HW/BW) ratio, larger heart cross-sectional area, and increased cardiomyocyte surface area. |
References: | |
| Cas No. | SDF | ||
| 分子式 | C77H120F3N25O19S2 | 分子量 | 1821.05 |
| 溶解度 | DMSO: 100 mg/mL (54.91 mM); Water: 33.33 mg/mL (18.30 mM) | 储存条件 | -20°C, protect from light |
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1 mg | 5 mg | 10 mg |
| 1 mM | 549.1 μL | 2.7457 mL | 5.4913 mL |
| 5 mM | 109.8 μL | 549.1 μL | 1.0983 mL |
| 10 mM | 54.9 μL | 274.6 μL | 549.1 μL |
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