1. Signaling Pathways
  2. GPCR/G Protein
  3. RXFP Receptor

RXFP Receptor (松弛素家族肽受体)

Relaxin family peptide

RXFP Receptor 是一类 G 蛋白偶联受体 (GPCRs),属于松弛素家族。该家族包括 RXFP1 (LGR7)、RXFP2 (LGR8)、RXFP3 (GPCR135) 和 RXFP4 (GPCR142)。 其上游配体有松弛素 (Relaxin)、胰岛素样肽 3 (INSL3)、松弛素-3 (Relaxin-3) 和胰岛素样肽 5 (INSL5) 等。下游涉及多个信号通路,如 cAMP、PI3K、MAPK 等信号通路。RXFP1 在生殖器官发育、组织纤维化调节、血管舒张等方面发挥作用;RXFP2 参与睾丸下降、生殖细胞存活和骨代谢等过程;RXFP3 可能与焦虑、食欲调节以及神经内分泌功能有关;RXFP4 的功能尚未完全明确,但与 INSL5 的作用相关联。RXFP1 与心脏和肾脏纤维化、哮喘、硬皮病以及胚胎植入异常密切相关;RXFP2 与隐睾症、不育症相关;RXFP3 在焦虑症和肥胖症的治疗方面具有潜在应用价值[1][2][3][4][5][6]

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].

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-156539
    RXFP1 receptor agonist-4
    RXFP1 receptor agonist-4 (Example 268) 是一种 RXFP1 受体 激动剂。RXFP1 receptor agonist-4 激活稳定表达人 RXFP1 的 HEK293 细胞中 cAMP 的产生,EC50 值为 4.9 nM。
    RXFP1 receptor agonist-4
  • HY-111583
    RXFP3/4 agonist 1
    RXFP3/4 agonist 1 是一种松弛素家族肽 3/4 受体 (RXFP3/4) 抑制剂,EC50 值分别为 82 和 2 nM。能够增强大鼠的食物摄取量。
    RXFP3/4 agonist 1
目录号 产品名 / 同用名 应用 反应物种