Efadirelaxin alfa
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.
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- CAS. Nr.: 3061442-66-5
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
Isotype
IgG1 Fc to human relaxin A
Species Reactivity
Human
IC50 & Target
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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.
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Cell Line:THP-1 human monocytic cells
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Concentration:0.075-1.2 nmol/L
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Incubation Time:2.5 h
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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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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]
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Dosage:30 mg/kg
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Administration:s.c.; twice weekly; 14 days
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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.
Conjugated
Unconjugated
Reconsititution
The product can be reconstituted/diluted with sterile PBS or saline.
Format
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G1-Fc_fragment-[PROT]2
Anwendung
ELISA, FACS, Functional assay
Chemical Information
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CAS. Nr. 3061442-66-5
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SMILES
[Efadirelaxin alfa]
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Synonyms
RELAX10
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Efadirelaxin alfa Related Classifications
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