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RXFP receptor agonists act on the four relaxin family peptide receptors, RXFP1 to RXFP4. Relaxin family peptide receptors (RXFP) are G protein-coupled receptors (GPCRs) for relaxin and insulin-like peptides. In 2002, the orphan leucine-rich repeat-containing G protein-coupled receptors 7 and 8 (LGR7, LGR8) were shown to respond to relaxin; they are now RXFP1 and RXFP2. RXFP3 is the receptor for relaxin-3, and RXFP4 binds insulin-like peptide 5. ML-290, reported in 2013, is a small-molecule RXFP1 agonist identified by high-throughput screening. B7-33 is a single-chain peptide derived from relaxin that activates RXFP1. AZD5462 is listed as an RXFP1 modulator, and A13:B7-24-GG is an RXFP4 agonist.
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.
B7-33 is a selective agonist for the relaxin receptor RXFP1, functioning as a single-chain relaxin mimetic. It promotes the phosphorylation of ERK1/2 while bypassing the activation of the cAMP signaling pathway. B7-33 displays significant anti-fibrotic and cardioprotective properties, making it a valuable tool in research focused on vascular diseases, including cardiomyopathy, myocardial infarction, and fibrosis.
RXFP2 Agonist 2 is a selective allosteric agonist of the RXFP2 receptor, exhibiting an EC50 of 0.38 μM. This compound promotes osteoblast mineralization and enhances bone formation in female mice. RXFP2 Agonist 2 is valuable for research studies focused on osteoporosis and bone health.
RXFP3/4 Agonist 2 is a potent nonpeptide dual agonist targeting RXFP3 and RXFP4, with EC50 values of 3.1 nM and 2.7 nM, respectively. This compound effectively promotes the interaction between RXFP3 and β-arrestin-2, displaying EC50 values ranging from 10 to 22 nM. RXFP3/4 Agonist 2 is valuable for investigating receptor signaling pathways and exploring potential therapeutic applications related to metabolic and cardiovascular diseases.
A13:B7-24-GG is a selective RXFP4 agonist that acts through its high-affinity binding (Ki = 2.29 nM) to the RXFP4 receptor, while demonstrating minimal interaction with RXFP3 (Ki = 602.56 nM). This compound effectively inhibits cAMP production with an EC50 of 1.17 nM and facilitates the recruitment of β-Arrestin2, showing an EC50 of 22.39 nM. A13:B7-24-GG is primarily utilized in research focused on chronic constipation and related gastrointestinal disorders.
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AZ7976 is a highly selective agonist for the Relaxin Family Peptide Receptor 1 (RXFP1), displaying a pEC50 value greater than 10.5. This compound enhances cAMP signaling through an allosteric mechanism, resulting in a physiological increase in heart rate. AZ7976 is suitable for investigations in cardiovascular disease research and related studies focusing on RXFP1-mediated pathways.
RXFP1 receptor agonist-6 is a potent agonist of the RXFP1 receptor, effectively stimulating cAMP production in HEK293 cells that stably express the human RXFP1. With an EC50 value of 12 nM, this compound is valuable for research applications focused on understanding RXFP1 signaling pathways and their implications in various physiological processes.
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RXFP2 Agonist 1 selectively targets the relaxin family peptide receptor 2 (RXFP2) and demonstrates potent agonistic activity with an EC50 of 0.06 µM. This compound plays a significant role in cellular signaling pathways associated with bone metabolism and has potential applications in osteoporosis research. Its ability to modulate RXFP2 activity makes it a valuable tool for studies focused on therapeutic strategies aimed at bone health and regeneration.
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RXFP1 receptor agonist-10 is a potent RXFP1 receptor agonist with an EC50 value of 0.5 nM. This compound exhibits significant biological activity, making it a valuable tool for studying the physiological roles of the RXFP1 receptor. Its utility in research extends to investigations related to heart failure, providing insights into the potential therapeutic mechanisms involving RXFP1 modulation.
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Synonyms: RELAX10
Efadirelaxin alfa is a selective agonist of the relaxin/insulin-like family peptide receptor RXFP1, exhibiting a prolonged terminal half-life following subcutaneous administration. It demonstrates significant anti-cardiac hypertrophy and anti-fibrotic properties by modulating the TGF-β1/Smad2 and AKT/eNOS signaling pathways. Efadirelaxin alfa effectively reverses cardiac hypertrophy and collagen deposition while improving cardiac systolic function, all without affecting blood pressure or heart rate. This compound is primarily utilized in research focused on heart failure mechanisms and therapies.
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RXFP1 receptor agonist-8 is a selective agonist for the RXFP1 receptor, which plays a crucial role in the modulation of cellular signaling pathways. This compound effectively stimulates cAMP production in HEK293 cells that stably express human RXFP1, exhibiting an EC50 value of 1.8 nM. It is valuable for research applications investigating RXFP1-mediated signaling and its physiological implications.
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RXFP3 Agonist 1 is a nonpeptide compound that selectively activates the RXFP3 receptor with an EC50 value of 6937 nM. This reagent is valuable for investigating the physiological roles of RXFP3 in various biological processes, including mood regulation and reproductive functions. Its application extends to studies exploring potential therapeutic targets for diseases associated with RXFP3 signaling pathways.
RXFP1 receptor agonist-4 is a selective agonist for the RXFP1 receptor. It effectively stimulates cyclic AMP (cAMP) production in HEK293 cells that stably express the human RXFP1 receptor, demonstrating an EC50 value of 4.9 nM. This compound is valuable for research applications related to the RXFP1 signaling pathway and its role in various physiological processes.
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RXFP1 receptor agonist-1 selectively targets the RXFP1 receptor, leading to the activation of downstream signaling pathways. This compound effectively stimulates cyclic AMP (cAMP) production in HEK293 cells that stably express human RXFP1, demonstrating an EC50 value of 300 nM. It serves as a valuable tool for research into receptor signaling mechanisms and the physiological implications of RXFP1 activation.
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RXFP1 receptor agonist-5 is a selective agonist for the RXFP1 receptor, a key regulator of various physiological processes. This compound effectively stimulates cAMP production in HEK293 cells that stably express the human RXFP1 receptor, demonstrating an EC50 value of 1.3 nM. It is an invaluable tool for research applications involving signal transduction, reproductive biology, and cardiovascular studies.
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Efranarelaxin alfa acts as a relaxin receptor agonist, primarily influencing cardiovascular health and tissue regeneration pathways. This compound has potential applications in research focused on cardiovascular diseases and promoting tissue repair mechanisms, offering a valuable tool for exploring therapeutic strategies in these areas.
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RXFP1 receptor agonist-3 is a selective agonist for the RXFP1 receptor, known to enhance the production of cyclic AMP (cAMP) in HEK293 cells that stably express the human RXFP1. With an effective concentration (EC50) of 2 nM, RXFP1 receptor agonist-3 serves as a valuable tool for studying the biological functions and signaling pathways associated with RXFP1, facilitating research in areas such as cardiovascular biology and neurobiology.
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RXFP1 receptor agonist-2 is a potent agonist of the RXFP1 receptor, demonstrating the ability to stimulate cAMP production in HEK293 cells stably expressing human RXFP1, with an EC50 value of 1 nM. This compound is useful for investigating the role of the RXFP1 receptor in various physiological processes and cellular signaling pathways. It serves as a valuable tool in pharmacological research focused on receptor function and related biological activities.
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RXFP1 receptor agonist-7 is a selective agonist of the RXFP1 receptor, facilitating significant increases in cAMP production. This compound has demonstrated an EC50 value of 4.2 nM in HEK293 cells stably expressing human RXFP1, indicating potent activity. RXFP1 receptor agonist-7 is suitable for research applications focusing on signal transduction, neurobiology, and cardiovascular studies involving the RXFP1 pathway.
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RXFP3/4 Agonist 1 is a selective agonist of the relaxin family peptide 3/4 receptors (RXFP3/4), exhibiting EC50 values of 82 nM for RXFP3 and 2 nM for RXFP4. This compound has been shown to enhance food intake in rat models, making it a valuable tool for studying appetite regulation and metabolic processes. Its potency and specificity make it suitable for research focusing on the roles of RXFP3/4 in energy homeostasis and related signaling pathways.
RXFP1 receptor agonist-9 is a selective agonist for the RXFP1 receptor, displaying an EC50 of 2.5 μM and a maximum response (Ymax) of 65%. This compound demonstrates excellent microsomal stability along with favorable pharmacokinetic properties, making it suitable for in vivo studies. RXFP1 receptor agonist-9 is primarily utilized in the investigation of heart failure and related cardiovascular conditions.
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