耗材描述
Teverelix
产品活性: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。
产品来源: https://www.medchemexpress.cn/teverelix.html
研究领域:GPCR/G Protein | Neuronal Signaling | Immunology/Inflammation
作用靶点:GnRH Receptor | Histamine Receptor
In Vitro: 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.
In Vivo: Teverelix (3-300 μg/kg, intramuscular injection) inhibits testosterone in rats.
Teverelix (1 mg/kg, s.c, daily for 3 days) abolishes luteal function in stumptailed macaques.
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