2. GPCR/G Protein PI3K/Akt/mTOR Immunology/Inflammation Protein Tyrosine Kinase/RTK
  3. RXFP Receptor Akt NO Synthase VEGFR
  4. Efadirelaxin alfa

Efadirelaxin alfa (RELAX10) 是一种高选择性的松弛素/胰岛素样家族肽受体 RXFP1 激活剂。Efadirelaxin alfa 在动物实验中经皮下给药后表现出显著延长的末端半衰期 (小鼠 7 天，大鼠 3.75 天)，且对 RXFP2、RXFP3 等相关受体无活性。Efadirelaxin alfa 具有显著的抗心肌肥厚和抗纤维化作用。Efadirelaxin alfa 能通过调节 TGF-β1/Smad2 及 AKT/eNOS 信号通路，有效减轻并逆转心肌肥厚及胶原沉积。Efadirelaxin alfa 改善心脏收缩功能的同时，并未引起血压或心率的波动，显示出良好的安全性。Efadirelaxin alfa 目前主要用于心力衰竭的相关研究。

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Efadirelaxin alfa

Efadirelaxin alfa Chemical Structure

CAS No. : 3061442-66-5

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Efadirelaxin alfa 相关抗体

Top Publications Citing Use of Products

查看 Akt 亚型特异性产品:

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Akt Akt1 Akt2 Akt3

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nNOS iNOS eNOS

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Efadirelaxin alfa (RELAX10) is a highly selective agonist of relaxin/insulin-like family peptide receptor RXFP1. After subcutaneous administration in animal experiments, Efadirelaxin alfa exhibits a significantly prolonged terminal half-life (7 days in mice, 3.75 days in rats), and shows no activity against related receptors such as RXFP2 and RXFP3. Efadirelaxin alfa has significant anti-cardiac hypertrophy and anti-fibrotic effects. Efadirelaxin alfa effectively attenuates and reverses cardiac hypertrophy and collagen deposition by regulating the TGF-β1/Smad2 and AKT/eNOS signaling pathways. Efadirelaxin alfa improves cardiac systolic function without causing fluctuations in blood pressure or heart rate, demonstrating favorable safety. Efadirelaxin alfa is currently mainly used in studies related to heart failure[1].

同型

IgG1 Fc to human relaxin A
反应种属

Human
IC50 & Target

eNOS

 

体外研究
(In Vitro)

Efadirelaxin alfa 在过表达 RXFP1 的 CHO-K1 细胞中特异性激活 RXFP1 介导的 cAMP 信号通路，IC50 为 1.94 nmol/L[1]。
Efadirelaxin alfa (0.075-1.2 nmol/L; 2.5 h) 可在人单核细胞 THP-1 中刺激 VEGF mRNA 水平升高 3 至 3.5 倍[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Efadirelaxin alfa 相关抗体:

Real Time qPCR[1]

Cell Line: THP-1 human monocytic cells
Concentration: 0.075-1.2 nmol/L
Incubation Time: 2.5 h
Result: Increased VEGF mRNA levels by 3- to 3.5-fold relative to no-treatment controls at all tested concentrations.
Showed no dose dependence in the evaluated range.
体内研究
(In Vivo)

Efadirelaxin alfa (30 mg/kg，皮下注射，每周 2 次) 可显著逆转 Isoprenaline (HY-B0468) 诱导已形成的心肌肥厚与纤维化的心肌肥厚，并抑制纤维化及促纤维化信号通路激活，同时增强有益的 AKT/eNOS 通路与蛋白质 S-亚硝基化通路[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J mice with Cardiac hypertrophy and fibrosis (male, 11 weeks old at study start, 15 mg/kg isoproterenol-induced via subcutaneous Alzet minipump)[1]
Dosage: 30 mg/kg
Administration: s.c.; twice weekly; 14 days
Result: Significantly attenuated isoproterenol-induced increases in heart weight/body weight, heart weight/tibial length, and cardiac collagen content.
Showed a trend toward improved ejection fraction and fractional shortening.
Significantly increased the ratios of phosphorylated (Ser1177)-endothelial NO synthase/total endothelial NO synthase and phosphorylated (Ser473)-protein kinase B/total protein kinase B.
Attenuated isoproterenol-induced increases in transforming growth factor β1 expression and phosphorylated Smad2/Smad ratio.
Increased myocardial protein S-nitrosylation, with additive increases when coadministered with isoproterenol.
应用

ELISA, FACS, Functional assay
偶联物

Unconjugated
复溶方法

The product can be reconstituted/diluted with sterile PBS or saline.
CAS 号
组分

Please refer to the lot-specific COA for specific buffer information.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Efadirelaxin alfa 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Efadirelaxin alfa3061442-66-5RELAX10RELAX 10RELAX-10RXFP ReceptorAktNO SynthaseVEGFRRelaxin family peptidePKBProtein kinase BNitric oxide synthasesNOSVascular endothelial growth factor receptorTHP-1 human monocytic cellsRXFP1CHO-K1 cellsRXFP2relaxin/insulin-like family peptide receptor 1heart failurecardiac hypertrophyADCYAP1R1RXFP4RXFP3Inhibitorinhibitorinhibit

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