RXFP Receptor Agonist

B7-33 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.

R2R01 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.

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.

A13:B7-24-GG is an engineered analogue of insulin-like peptide 5 (INSL5), a selective RXFP4 agonist with a K_i value of 2.29 nM. A13:B7-24-GG has an extremely low binding affinity for RXFP3 (K_i = 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.

RXFP1 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.

Efranarelaxin alfa is a relaxin receptor agonist. Efranarelaxin alfa is promising for research of cardiovascular diseases and tissue repair.