Degarelix
同義詞：地加瑞克
分子量：1632.26
分子式：C82H103ClN18O16
CAS 號(hào)：214766-78-6
產(chǎn)品描述：
Degarelix 是一種競(jìng)爭(zhēng)性的、可逆的促性腺激素釋放激素受體 (GnRHR/LHRHR) 拮抗劑。Degarelix 可用于前列腺癌的研究。
體外研究：
Degarelix shows only very weak histamine-releasing properties and the lowest capacity for histamine release among the antagonists of LHRH, including Cetrorelix (HY-P0009), Abarelix (HY-13534), and Ganirelix (HY-P1628)。
Degarelix (1 nM-10 μM, 0-72 h) reduces cell viability in all prostate cell lines (WPE1-NA22, WPMY-1, BPH-1, VCaP cells), with the exception of the PC-3 cells。
Degarelix (10 μM, 0-72 h) exerts a direct effect on prostate cell growth through apoptosis。
體內(nèi)研究:
Degarelix (0-10 μg/kg; s.c.; once) decreases plasma LH levels and plasma testosterone levels in a dose-dependent manner in castrated rats.
Degarelix is stable when incubated in microsomes and cryopreserved hepatocytes from animal liver tissue. In rat and dog, most of the degarelix dose is eliminated within 48 h via urine and feces in equal amounts (40–50% in each matrix), whereas in monkey the major route of excretion is fecal (50%) and renal (22%).
