CetRORelix 是一种GnRH受体的强效拮抗剂(IC50:1.21 nM)。
产品描述
Cetrorelix Acetate is gonadotropin-releasing hormone (GnRH) receptor antagonist with an IC50 of 1.21 nM.
体外活性
GnRH-I antagonist Cetrorelix inhibited growth of ES-2 cell line only at 1000 ng/ml.?The incubation of ES-2 ovarian cancer cells in vitro with an GnRH-I antibody inhibited cell proliferation in a time and concentration-dependent manner.?GnRH-I may function as an autocrine growth factor in this ovarian cancer cell line [1].
体内活性
Cetrorelix inhibits the activation of hGnRHR and a downstream luciferase reporter gene in murine LTK- cells by the GnRHR agonist [D-Trp6]GnRH (IC50 = 1.2 nM). In vivo, cetrorelix (60 μg per day) reduces tumor volume to 35% of control and decreases serum luteinizing hormone levels by 50% in a human epithelial ovarian cancer mouse xenograft model[2].
Cas No.
145672-81-7
分子式
C72H96ClN17O16
分子量
1491.11
别名
Cetrorelix;醋酸西曲瑞克
储存和溶解度
DMSO:50 mg/mL (33.53 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years