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Degarelix acetate(214766-78-6 free base)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Degarelix acetate(214766-78-6 free base)图片
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议

产品介绍
Degarelix acetate(214766-78-6 free base) 是促性腺激素释放激素受体 (GnRHR) 的竞争性可逆拮抗剂。

产品描述

Degarelix acetate is a competitive and reversible antagonist of gonadotropin-releasing hormone receptor (GnRHR) .

体外活性

Degarelix directly acts on the pituitary receptors to luteinizing hormone-releasing hormone (LHRH), preventing the effect of endogenous LHRH. The use of degarelix eliminates the undesirable surge of initial gonadotropin and testosterone levels produced by LHRH agonists. With the exception of PC-3 cells, Degarelix treatment reduces the cell viability of all prostate cell lines (WPE1-NA22, WPMY-1, BPH-1 cells, VCaP cells). GnRH antagonist degarelix has a direct effect on the growth of prostate cells through apoptosis.

体内活性

In a single subcutaneous injection of 0.3 to 10 μg/kg in rats, degarelix produced a dose-dependent inhibition of the pituitary-gonad axis as revealed by the decrease in plasma luteinizing hormone (LH) and testosterone levels. The duration of LH inhibition increased with increasing dose: in rats, after subcutaneous injection of digarelix 12.5, 50 or 200 μg/kg, the significant inhibition of LH lasted 1, 2 and 7 days, respectively [ 3]. Degarelix is stable when incubated in microsomes and liver cells cryopreserved in animal liver tissue.

Cas No.

T10988L

分子式

C84H107ClN18O18

分子量

1692.34

储存和溶解度

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years