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Degarelix acetate hydrate
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 hydrate图片
CAS NO:934246-14-7
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
地加瑞克醋酸水合物
产品介绍
Degarelix acetate hydrate 是一种竞争性的、可逆的促性腺激素释放激素受体 (GnRHR/LHRHR) 拮抗剂。Degarelix acetate hydrate 可用于前列腺癌的研究。
生物活性

Degarelix acetate hydrate is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR/LHRHR) antagonist. Degarelix acetate hydrate can be used for prostatecancerresearch[1].

体外研究
(In Vitro)

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)[1].
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[2].
Degarelix (10 μM, 0-72 h) exerts a direct effect on prostate cell growth through apoptosis[2].

Cell Viability Assay[2]

Cell Line:WPMY-1, WPE1-NA22, BPH-1, LNCaP and VCaP
Concentration:1 nM-10 μM
Incubation Time:WPMY-1 cells at 48 and 72h, WPE1-NA22 cells at 72 hours, BPH-1 cells at 48 and 72h, LNCaP cells at 48 and 72h
Result:Reduced cell viability in all prostate cell lines, with the exception of the PC-3 cells.

Apoptosis Analysis[2]

Cell Line:WPE1-NA22, BPH-1, LNCaP and VCaP
Concentration:10 μM
Incubation Time:24, 48 and 72 h
Result:Induced a significant increase on caspase 3/7 activation.
体内研究
(In Vivo)

Degarelix (0-10 μg/kg; s.c.; once) decreases plasma LH levels and plasma testosterone levels in a dose-dependent manner in castrated rats[3].
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%)[4].

Animal Model:Male Sprague-Dawley rats, castrated[3]
Dosage:0.3, 1, 3 and 10 μg/kg or 12.5, 50, and 200 μg/kg
Administration:Subcutaneous injection, once
Result:Produced a dose-dependent and reversible decrease in plasma LH levels with a minimal effective dose of 3 μg/kg.
For the 50 μg/kg and 200 μg/kg doses, t1/2of absorption values were 4 min and 30 min, Tmaxvalues were 1 h and 5 h, and apparent plasma disappearance t1/2values were 12 h and 67 h, respectively.
Produced a dose-dependent decrease in plasma testosterone levels with a minimal effective dose of 1 μg/kg.
Clinical Trial
Formula

C82H103ClN18O16.xC2H4O2.xH2O

CAS 号

934246-14-7

中文名称

地加瑞克醋酸水合物

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.