RXFP receptor

AZD5462 is a potent orally available relaxin receptor RXFP1 agonist for the study of heart failure and cancer.

RXFP3/4 agonist 2 is a potent, non-peptidic bis-RXFP3/4 agonist that facilitates the interaction between RXFP3 and β-arrestin-2 and is useful for studying diseases caused by metabolic abnormalities.

RLX-33 is a potent and selective antagonist of relaxin family peptide 3 (RXFP3) that crosses the blood-brain barrier and also blocks relaxin 3-induced ERK1/2 phosphorylation. RLX-33 can block the increase in food intake induced by the RXFP3 selective agonist R3/I5 in rats.RLX-33 can be used to study the metabolic syndrome.

Efranarelaxin alfa is an agonist of the relaxin receptor. It shows potential for research in cardiovascular diseases and tissue repair.

RXFP1 receptor agonist-5 (Example 98) is an agonist targeting the RXFP1 receptor, inhibiting cAMP production in HEK293 cells with stable human RXFP1 expression, with an EC50 of 1.3 nM [1].

RXFP1 receptor agonist-4 (Example 268) is a potent RXFP1 receptor agonist, shown to effectively suppress cAMP production in HEK293 cells stably expressing the human RXFP1 receptor, with an effective concentration (EC50) of 4.9 nM [1].

Relaxin H3 (human) (TFA) is a relaxin peptide that exerts antifibrotic effects through the RXFP1 receptor.

B7-33 is a single-chain relaxin analog and a selective agonist for relaxin receptor 1 (RXFP1). It binds to RXFP1 and preferentially activates the pERK pathway in cells expressing RXFP1, rather than cAMP. B7-33 serves as an antifibrotic agent and provides cardioprotective effects.

AZ7976 (Compound 42), a potent and highly selective agonist for Relaxin Family Peptide Receptor 1 (RXFP1) with a pEC 50 value greater than 10.5, operates through an allosteric mechanism to enhance RXFP1's cAMP signaling, which physiologically elevates heart rate. This property makes AZ7976 a valuable tool in cardiovascular disease research [1].

RXFP1 receptor agonist-1 (Example 2), suppresses cAMP production in HEK293 cells constitutively expressing the human RXFP1, with an EC50 of 300 nM [1].

ML-290 is an effective relaxin/insulin-like family peptide receptor (RXFP1) agonist and activator of anti-fibrotic genes. It shows an EC50 of 94 nM.

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

RXFP3/4 agonist 1 is a relaxin family peptide 3/4 receptor (RXFP3/4) agonist(EC50s of 82/2 nM, respectivley).

Example 2 (RXFP1 receptor agonist-8) is a potent RXFP1 receptor agonist that suppresses cAMP production in HEK293 cells expressing human RXFP1, exhibiting an EC50 of 1.8 nM [1].

RXFP1 receptor agonist-7 (Example 2) is an RXFP1 receptor agonist that effectively inhibits cAMP production in HEK293 cells stably expressing the human RXFP1, with an EC50 of 4.2 nM [1].

RXFP1 Receptor Agonist-2 (Example 124), an EC50 value of 1 nM [1].

Relaxin H3 (human), a relaxin peptide, exhibits antifibrotic effects by activating RXFP1 [1].

RXFP1 receptor agonist-6 (Example 7) acts as an agonist for the RXFP1 receptor and effectively suppresses cAMP production in HEK293 cells stably expressing the human RXFP1, with an EC50 of 12 nM [1].

RXFP1 receptor agonist-3 (Example 223) is an RXFP1 receptor agonist that inhibits cyclic AMP (cAMP) production in HEK293 cells stably expressing human RXFP1, with an EC50 of 2 nM [1].