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].
References:
- [1]. Kong RC, et al. Membrane receptors: structure and function of the relaxin family peptide receptors. Mol Cell Endocrinol. 2010 May 14;320(1-2):1-15. [Content Brief]
- [2]. Halls ML, et al. Relaxin family peptide receptors--former orphans reunite with their parent ligands to activate multiple signalling pathways. Br J Pharmacol. 2007 Mar;150(6):677-91. [Content Brief]
- [3]. Bennett R, et al. ODP010 Relaxin Receptor RXFP1 Knockout in Adipose Tissue Progenitor Cells Results in Resistance to High Fat Diet-Induced Weigh Gain. Journal of the Endocrine Society, 2022, 6(Supplement_1): A11-A12.
- [4]. Zhang C, et al. Central relaxin-3 receptor (RXFP3) activation reduces elevated, but not basal, anxiety-like behaviour in C57BL/6J mice. Behav Brain Res. 2015 Oct 1;292:125-32. [Content Brief]
- [5]. Halls ML, et al. Relaxin family peptide receptors RXFP1 and RXFP2 modulate cAMP signaling by distinct mechanisms. Mol Pharmacol. 2006 Jul;70(1):214-26. [Content Brief]
- [6]. Lian X, et al. RXFP1 Receptor Activation by Relaxin-2 Induces Vascular Relaxation in Mice via a Gαi2-Protein/PI3K?/γ/Nitric Oxide-Coupled Pathway. Front Physiol. 2018 Sep 4;9:1234. [Content Brief]
All Product Categories
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RXFP Receptor Related Products (28)
Related Products (28)
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Antibodies (1)
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Efranarelaxin alfa
0 ImagesCat. No.: HY-P991133CAS No.: 2969217-22-7Efranarelaxin alfa is a relaxin receptor agonist. Efranarelaxin alfa is promising for research of cardiovascular diseases and tissue repair.
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RXFP1 receptor agonist-3
0 ImagesCat. No.: HY-156538CAS No.: 2924767-53-1RXFP1 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.
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Relaxin H3 (human)
0 ImagesCat. No.: HY-P4890CAS No.: 1158181-62-4Relaxin H3 (human) is a relaxin peptide with anti-inflammatory, anti-apoptotic, anti-pyroptotic, anti-migratory, protective and anti-fibrotic activities. Relaxin H3 (human) acts on RXFP1 to generate cAMP and reduce the levels of ATP and ROS. Relaxin H3 (human) inhibits renal inflammatory pyroptosis (pyroptosis), NLRP3 inflammasome activation, caspase-1 activation, IL-1β/IL-18 secretion, collagen synthesis, TGF-β1 signaling pathway, Smad2 phosphorylation, myofibroblast differentiation, TIMP expression, and HRMEC migration. Relaxin H3 (human) activates AMPK, upregulates MFN2 expression, improves mitochondrial quality control and membrane potential, inhibits apoptosis (apoptosis) and pyroptosis, restores retinal ultrastructure, and reverses excessive left ventricular collagen expression. Relaxin H3 (human) can be used in studies related to kidney stones, nephrocalcinosis, diabetic cardiomyopathy, fibrotic cardiomyopathy, and diabetic retinopathy.
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RXFP1 receptor agonist-2
0 ImagesCat. No.: HY-156537CAS No.: 2924460-54-6RXFP1 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.
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RXFP1 receptor agonist-7
0 ImagesCat. No.: HY-156542CAS No.: 2941484-13-3RXFP1 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.
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RXFP3/4 agonist 1
0 ImagesCat. No.: HY-111583CAS No.: 2351104-40-8RXFP3/4 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.
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Efadirelaxin alfa
0 ImagesCat. No.: HY-P992108CAS No.: 3061442-66-5Synonyms: RELAX10Efadirelaxin 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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RXFP1 receptor agonist-9
0 ImagesCat. No.: HY-174334CAS No.: 2924765-23-9RXFP1 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.
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