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 No.: 3061442-66-5
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Biological Activity
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Chemical Information
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Biological Activity
IgG1 Fc to human relaxin A
Human
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eNOS |
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.
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.
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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G1-Fc_fragment-[PROT]2
ELISA, FACS, Functional assay
Chemical Information
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CAS No. 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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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Efadirelaxin alfa Related Classifications
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