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 Agonists (2)

RXFP Receptor Related Products (20)
Antibodies (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-112606

ML-290		99.81%
ML-290 is a first-in-class and potent relaxin/insulin-like family peptide receptor (RXFP1) agonist and activator of anti-fibrotic genes, with an EC₅₀ of 94 nM. ML290 is a biased allosteric agonist at the relaxin receptor RXFP1.

HY-148087

AZD5462		99.88%
AZD5462 is a RXFP1 modulator, can be used for heart failure research. RXFP1 is the cognate receptor for human relaxin, belongs to GPCR family 1c number with anti-fibrotic and anti-inflammatory properties.

HY-145278

RXFP3/4 agonist 2		99.82%
RXFP3/4 agonist 2 is a potent, nonpeptide dual RXFP3/4 agonist (EC₅₀=3.1 and 2.7 nM). RXFP3/4 agonist 2 also potently promotes interactions between RXFP3 and β-arrestin-2 with EC₅₀ values in the range of 10-22 nM.

HY-150186

RXFP2 agonist 2
RXFP2 agonist 2 is a selective，orally active and allosteric RXFP2 agonist with an EC₅₀ value of 0.38 µM. RXFP2 agonist 2 induces osteoblast mineralization. RXFP2 agonist 2 increases bone formation in female mice. RXFP2 agonist 2 has the potential for the research of osteoporosis.

HY-P4890A

Relaxin H3 (human) (TFA)
Relaxin H3 (human) (TFA) is a kind of relaxin peptide. Relaxin H3 (human) (TFA) exerts antifibrotic actions via RXFP1.

HY-P10687

H3B10-27(13/17αF)
H3B10-27(13/17αF) is an excellent scaffold for further developing reagent candidates and an important tool for understanding the physiological functions of the neuropeptide G protein-coupled receptor RXFP3, and it's very stable in serum.

HY-P10728

B7-33	Agonist
B7-33 is a single-chain relaxin mimetic. B7-33 is a selective relaxin receptor 1 (RXFP1) agonist. B7-33 binds to RXFP1 and preferentially activates thepERK pathway over cAMP in cells (with RXFP1 expression). B7-33 is an anti-fibrotic agent. B7-33 has cardioprotective effects.

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-162401

AZ7976	Agonist
AZ7976 (Compound 42) is a highly selective agonist for the Relaxin Family Peptide Receptor 1 (RXFP1) (pEC₅₀ > 10.5). AZ7976 enhances RXFP1's cAMP signaling through an allosteric mechanism, thereby physiologically increasing heart rate. AZ7976 can be used in the field of cardiovascular disease research.

HY-156541

RXFP1 receptor agonist-6
RXFP1 receptor agonist-6 (Example 7) is a RXFP1 receptor agonist. RXFP1 receptor agonist-6 stimulates cAMP production in HEK293 cells stably expressing human RXFP1, with an EC₅₀ value of 12 nM.

HY-150185

RXFP2 agonist 1
RXFP2 agonist 1 (Compound 1715) is a potent RXFP2 agonist with an EC₅₀ value of 0.06 µM. RXFP2 agonist 1 has the potential for the research of osteoporosis.

HY-156543

RXFP1 receptor agonist-8
RXFP1 receptor agonist-8 (Example 2) is a RXFP1 receptor agonist. RXFP1 receptor agonist-8 stimulates cAMP production in HEK293 cells stably expressing human RXFP1, with an EC₅₀ value of 1.8 nM.

HY-145279

RXFP3 agonist 1
RXFP3 agonist 1 is a nonpeptide RXFP3 agonist (EC₅₀=6937 nM).

HY-156539

RXFP1 receptor agonist-4
RXFP1 receptor agonist-4 (Example 268) is a RXFP1 receptor agonist. RXFP1 receptor agonist-4 stimulates cAMP production in HEK293 cells stably expressing human RXFP1, with an EC₅₀ value of 4.9 nM.

HY-156536

RXFP1 receptor agonist-1
RXFP1 receptor agonist-1 (Example 2 peak2) is a RXFP1 receptor agonist. RXFP1 receptor agonist-1 stimulates cAMP production in HEK293 cells stably expressing human RXFP1, with an EC₅₀ value of 300 nM.

HY-156540

RXFP1 receptor agonist-5
RXFP1 receptor agonist-5 (Example 98) is a RXFP1 receptor agonist. RXFP1 receptor agonist-5 stimulates cAMP production in HEK293 cells stably expressing human RXFP1, with an EC₅₀ value of 1.3 nM.

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.

HY-P4890

Relaxin H3 (human)
Relaxin H3 (human) is a kind of relaxin peptide. Relaxin H3 (human) exerts antifibrotic actions via RXFP1.

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.

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.

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RXFP Receptor

RXFP Receptor Related Products (20)

Antibodies (1)

RXFP Receptor Related Products (20):