| Bioactivity | Degarelix acetate (FE 200486) is a decapeptide that shows high affinity/selectivity to human gonadotropin-releasing hormone (GnRH) receptor (IC50 = 3 nM). Degarelix acetate (FE 200486) is used for the research of prostate cancer[1][2]. |
| Invitro | Degarelix (FE 200486) 有非常弱的组胺释放特性，并且在所有 LHRH 拮抗剂中，包括 Cetrorelix (HY-P0009)、Abarelix (HY-13534) 和 Ganirelix (HY-P1628)，其组胺释放能力最低[1]。Degarelix (1 nM-10 μM, 0-72 小时) 会降低所有前列腺细胞系 (WPE1-NA22, WPMY-1, BPH-1, VCaP 细胞) 的细胞活力，PC-3 细胞除外[4]。Degarelix (10 μM, 0-72 小时) 通过诱导凋亡直接影响前列腺细胞生长[4]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Degarelix acetate 相关抗体: Cell Viability Assay[4] Cell Line: |
| In Vivo | Degarelix (FE 200486 free base) (0-10 μg/kg; 皮下注射; 一次) 以剂量依赖性方式降低去势大鼠的血浆 LH 水平和血浆睾酮水平[5]。Degarelix (FE 200486 free base) 在动物肝脏组织的微粒体和冷冻保存的肝细胞中培养时是稳定的。在大鼠和狗中，大部分 Degarelix 剂量在 48 小时内通过尿液和粪便以相等的量（每种基质 40-50%）排泄，而在猴子中，主要的排泄途径是粪便 (50%) 和肾脏 (22%)[6]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| CAS | 934016-19-0 |
| Formula | C84H107ClN18O18 |
| Molar Mass | 1692.31 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Anders Sonesson, et al. In Vitro and In Vivo Human Metabolism of Degarelix, a Gonadotropin-Releasing Hormone Receptor Blocker. Drug Metabolism and Disposition. July 2013, 41 (7) 1339-1346. [2]. Degarelix. [3]. Rick FG, et al. An update on the use of degarelix in the treatment of advanced hormone-dependent prostate cancer. Onco Targets Ther. 2013 Apr 16;6:391-402. [4]. Sakai M, et al. In search of the molecular mechanisms mediating the inhibitory effect of the GnRH antagonistdegarelix on human prostate cell growth. PLoS One. 2015 Mar 26;10(3):e0120670. [5]. Broqua P, et al. Pharmacological profile of a new, potent, and long-acting gonadotropin-releasing hormoneantagonist: degarelix. J Pharmacol Exp Ther. 2002 Apr;301(1):95-102. [6]. Sonesson A, et al. Metabolite profiles of degarelix, a new gonadotropin-releasing hormone receptor antagonist, in rat, dog, and monkey. Drug Metab Dispos. 2011 Oct;39(10):1895-903. |
Degarelix acetate
CAS: 934016-19-0 F: C84H107ClN18O18 W: 1692.31
Degarelix acetate (FE 200486) is a decapeptide that shows high affinity/selectivity to human gonadotropin-releasing horm
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This product is for research use only, not for human use. We do not sell to patients.