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  (Synonyms: RELAX10)

Cat. No.: HY-P992108
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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.

For research use only. We do not sell to patients.

Efadirelaxin alfa

Efadirelaxin alfa Chemical Structure

CAS No. : 3061442-66-5

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Efadirelaxin alfa Related Antibodies

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

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Description

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].

Isotype

IgG1 Fc to human relaxin A
Species Reactivity

Human
IC50 & Target

eNOS

 

In Vitro

Efadirelaxin alfa specifically activates the RXFP1-mediated cAMP signaling pathway in CHO-K1 cells overexpressing RXFP1, with an IC50 of 1.94 nmol/L[1].
Efadirelaxin alfa (0.075-1.2 nmol/L; 2.5 h) stimulates a 3- to 3.5-fold increase in VEGF mRNA levels in the human monocyte cell line THP-1[1].

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

Efadirelaxin alfa Related Antibodies

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.
In Vivo

Efadirelaxin alfa (30 mg/kg, subcutaneous injection, twice weekly) significantly reverses established myocardial hypertrophy induced by Isoprenaline (HY-B0468), inhibits myocardial fibrosis and the activation of profibrotic signaling pathways, and simultaneously enhances the beneficial AKT/eNOS pathway and protein S-nitrosylation pathway[1].

MedChemExpress (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.
Application

ELISA, FACS, Functional assay
Conjugated

Unconjugated
Reconsititution

The product can be reconstituted/diluted with sterile PBS or saline.
CAS No.
SMILES

[Efadirelaxin alfa]
Formulation

Please refer to the lot-specific COA for specific buffer information.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Efadirelaxin alfa Related Classifications

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Help & FAQs
  • 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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