2. Signaling Pathways
  3. GPCR/G Protein
  4. RXFP Receptor

RXFP Receptor

Relaxin family peptide

RXFP Receptor is a type of G protein-coupled receptor (GPCRs) and belongs to the relaxin family. The family includes RXFP1 (LGR7), RXFP2 (LGR8), RXFP3 (GPCR135) and RXFP4 (GPCR142). Its upstream ligands include relaxin, insulin-like peptide 3 (INSL3), relaxin-3 (Relaxin-3) and insulin-like peptide 5 (INSL5). Multiple signaling pathways are involved downstream, such as cAMP, PI3K, MAPK and other signaling pathways. RXFP1 plays a role in reproductive organ development, tissue fibrosis regulation, vasodilation, etc.; RXFP2 is involved in testicular descent, germ cell survival and bone metabolism; RXFP3 may be related to anxiety, appetite regulation and neuroendocrine function; the function of RXFP4 has not yet been fully clarified, but it is associated with the role of INSL5. RXFP1 is closely related to cardiac and renal fibrosis, asthma, scleroderma, and abnormal embryo implantation; RXFP2 is associated with cryptorchidism and infertility; RXFP3 has potential application value in the treatment of anxiety and obesity[1][2][3][4][5][6].

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P991133
    Efranarelaxin alfa
    		Agonist
    Efranarelaxin alfa is a relaxin receptor agonist. Efranarelaxin alfa is promising for research of cardiovascular diseases and tissue repair.
    Efranarelaxin alfa
  • HY-156538
    RXFP1 receptor agonist-3
    RXFP1 receptor agonist-3 (Example 223) is a RXFP1 receptor agonist. RXFP1 receptor agonist-3 stimulates cAMP production in HEK293 cells stably expressing human RXFP1, with an EC50 value of 2 nM.
    RXFP1 receptor agonist-3
  • HY-P4890
    Relaxin H3 (human)
    Relaxin H3 (human) is a kind of relaxin peptide. Relaxin H3 (human) exerts antifibrotic actions via RXFP1.
    Relaxin H3 (human)
  • HY-156537
    RXFP1 receptor agonist-2
    RXFP1 receptor agonist-2 (Example 124) is a RXFP1 receptor agonist. RXFP1 receptor agonist-2 stimulates cAMP production in HEK293 cells stably expressing human RXFP1, with an EC50 value of 1 nM.
    RXFP1 receptor agonist-2
  • HY-156542
    RXFP1 receptor agonist-7
    RXFP1 receptor agonist-7 (Example 2) is a RXFP1 receptor agonist. RXFP1 receptor agonist-7 stimulates cAMP production in HEK293 cells stably expressing human RXFP1, with an EC50 value of 4.2 nM.
    RXFP1 receptor agonist-7
  • HY-111583
    RXFP3/4 agonist 1
    RXFP3/4 agonist 1 is an agonist of relaxin family peptide 3/4 receptor (RXFP3/4), with EC50s of 82/2 nM, respectivley. RXFP3/4 agonist 1 increases food intake in rats.
    RXFP3/4 agonist 1
  • HY-P992108
    Efadirelaxin alfa
    		Activator
    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.
    Efadirelaxin alfa
  • HY-174334
    RXFP1 receptor agonist-9
    		Inhibitor
    RXFP1 receptor agonist-9 is a potent RXFP1 agonist with an EC50 of 2.5 μM and Ymax of 65%. RXFP1 receptor agonist-9 exhibits good microsomal stability, reasonable PK and pharmacological activity. RXFP1 receptor agonist-9 can be used to the study of heart failure.
    RXFP1 receptor agonist-9
Cat. No. Product Name / Synonyms Application Reactivity