- Signaling Pathways
- GPCR/G Protein
- RXFP Receptor
RXFP Receptor
Relaxin family peptide
- [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]
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RXFP Receptor Related Products (28)
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Antibodies (1)
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ML-290
0 ImagesML-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. -
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AZD5462
0 ImagesAZD5462 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. -
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RXFP3/4 agonist 2
0 ImagesRXFP3/4 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. -
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B7-33
0 ImagesB7-33 is a single-chain relaxin mimetic and a selective relaxin receptor 1 (RXFP1) agonist. B7-33 phosphorylates ERK1/2 without inducing activation of the cAMP signaling pathway. B7-33 exhibits anti-fibrotic and cardioprotective activities. B7-33 can be used in the research of vascular diseases such as cardiomyopathy, myocardial infarction and fibrosis. -
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Relaxin H3 (human) TFA
0 ImagesCat. No.: HY-P4890ARelaxin H3 (human) TFA is a relaxin peptide with anti-inflammatory, anti-apoptotic, anti-pyroptotic, anti-migratory, protective and anti-fibrotic activities. Relaxin H3 (human) TFA acts on RXFP1 to generate cAMP and reduce the levels of ATP and ROS. Relaxin H3 (human) TFA 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) TFA 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) TFA can be used in studies related to kidney stones, nephrocalcinosis, diabetic cardiomyopathy, fibrotic cardiomyopathy, and diabetic retinopathy. -
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Anti-LGR7 Antibody
0 ImagesCat. No.: HY-P992258 -
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R9-13
0 ImagesCat. No.: HY-P11625R9-13 is a fatty acid-conjugated relaxin and an agonist of LGR7 (RXFP1). R9-13 induces sustained pubic symphysis elongation in estrogen-pretreated mice. R9-13 exhibits long-acting pharmacokinetic profiles in rodents, with in vivo activity lasting up to one week after administration. R9-13 can be used in studies related to acute heart failure. -
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R2R01
0 ImagesCat. No.: HY-P11619R2R01 is a potent and selective relaxin family peptide receptor 1 (RXFP1) agonist with an EC50 of 0.34 nM. R2R01 activates RXFP1 to induce relaxin-like biological responses. R2R01 can increase heart rate in pithed and conscious rats. R2R01 can be used for the research of cardiovascular diseases. -
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RXFP2 agonist 2
0 ImagesCat. No.: HY-150186CAS No.: 2971704-85-3RXFP2 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. -
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AZ7976
0 ImagesCat. No.: HY-162401CAS No.: 2813866-27-0AZ7976 (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. -
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RXFP1 receptor agonist-6
0 ImagesCat. No.: HY-156541CAS No.: 2941346-85-4RXFP1 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. -
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- H3B10-27(13/17αF)
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RXFP2 agonist 1
0 ImagesCat. No.: HY-150185CAS No.: 2971704-58-0RXFP2 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. -
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A13:B7-24-GG
0 ImagesCat. No.: HY-P11246CAS No.: 3057097-31-8A13:B7-24-GG is an engineered analogue of insulin-like peptide 5 (INSL5), a selective RXFP4 agonist with a Ki value of 2.29 nM. A13:B7-24-GG has an extremely low binding affinity for RXFP3 (Ki = 602.56 nM) and an inhibitory effect on cAMP (EC50) of 1.17 nM. Activation of RXFP4 by A13:B7-24-GG leads to the recruitment of β-Arrestin2, with an EC50 of 22.39 nM. A13:B7-24-GG can be used for research on chronic constipation. -
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RXFP1 receptor agonist-10
0 ImagesCat. No.: HY-176215CAS No.: 2924450-63-3RXFP1 receptor agonist-10 (Compound 188) is a RXFP1 receptor agonist (EC50: 0.5 nM). RXFP1 receptor agonist-10 can be used for research of heart failure. -
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RXFP1 receptor agonist-8
0 ImagesCat. No.: HY-156543CAS No.: 2941271-76-5RXFP1 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. -
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RXFP3 agonist 1
0 ImagesCat. No.: HY-145279CAS No.: 2752378-24-6RXFP3 agonist 1 is a nonpeptide RXFP3 agonist (EC50=6937 nM). -
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RXFP1 receptor agonist-4
0 ImagesCat. No.: HY-156539CAS No.: 2941376-76-5RXFP1 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. -
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RXFP1 receptor agonist-1
0 ImagesCat. No.: HY-156536CAS No.: 2924619-64-5RXFP1 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. -
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RXFP1 receptor agonist-5
0 ImagesCat. No.: HY-156540CAS No.: 2941385-36-8RXFP1 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. -
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