Teverelix (EP 24332) 是一种GnRH拮抗剂。Teverelix 可竞争性和可逆性地与GnRH受体 (GnRH receptors) 结合,从而抑制LH和FSH的释放。Teverelix可用于前列腺增生、子宫内膜异位症和前列腺癌的研究。
Teverelix (10 nM, 45 mins) inhibits GnRH-induced intracellular Ca2+ increase in HEK293/GnRHR cells。
Teverelix (0.1 nM-1 μM, 45 mins) inhibits GnRH-induced cAMP accumulation in HEK293/GnRHR cells。
Teverelix (10 nM-1 μM, 15 mins) inhibits GnRH-induced pERK1/2 and pCREB activation in HEK293/GnRHR cells。
Teverelix inhibits histamine release in a peritoneal rat mast cell, with an EC50value of 81 μg/mL
分子量:1459.13
分子式:C74H100ClN15O14
CAS 号 151272-78-5
参考文献:
GnRH Antagonists Produce Differential Modulation of the Signaling Pathways Mediated by GnRH Receptors【DOI: 10.3390/ijms20225548】