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]

RXFP Receptor Related Products (23)
Antibodies (1)

By Effects:	Inhibitor (1) Agonists (4)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

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.

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.

HY-174334

RXFP1 receptor agonist-9	Inhibitor
RXFP1 receptor agonist-9 is a potent RXFP1 agonist with an EC₅₀ of 2.5 μM and Y_max 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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RXFP Receptor

RXFP Receptor Related Products (23)

Antibodies (1)

RXFP Receptor Related Products (23):