FSHR agonist 1

Names

[ CAS No. ]:
1256776-89-2

[ Name ]:
FSHR agonist 1

Biological Activity

[Description]:

FSHR agonist 1 is a high affinity and allosteric follicle stimulating hormone receptor (FSHR) agonist with a pEC50 of 7.72. FSHR agonist 1 formes extensive interactions with the TMD to directly activate FSHR[1].

[Related Catalog]:

Signaling Pathways >> Others >> Estrogen Receptor/ERR
Research Areas >> Endocrinology

[Target]

pEC50: 7.72 (FSHR)[1]


[In Vitro]

FSHR agonist 1 (compound 21f) 与 FSHR TMD 口袋的结合诱导 TM6 和 TM7 向内运动，这直接导致 FSHR 激活[1]。 FSHR agonist 1 (compound 21f) 可以高效激活 FSHR、LHCGR 和 TSHR，而对 FSHR 的激活效力比 LHCGR（pEC50 为 6.26）和 TSHR（pEC50 为 6.48）高 10 倍以上[1]。

[References]

[1]. Jia Duan, et al. Universal mechanism of hormone and allosteric agonist mediated activation of glycoprotein hormone receptors as revealed by structures of follicle stimulating hormone receptor. biorxiv. August 01, 2022.

Chemical & Physical Properties

[ Molecular Formula ]:
C26H33N3O3S

[ Molecular Weight ]:
467.62

Related Compounds