120287-85-6

• 常用中文名：西曲瑞克
• 常用英文名：Antide acetate salt
• CAS号：120287-85-6
• 分子式：C₇₀H₉₂ClN₁₇O₁₄
• 分子量：1431.038
• 相关类别： 原料药 激素及调节内分泌功能类药 促性激素类药
• 发布时间：2018-08-30 21:57:20
• 更新时间：2024-01-02 18:06:42
• 西曲利是一种有效的促性腺激素释放激素(GnRH)拮抗剂。西曲利抑制卵巢刺激期间内源性黄体生成激素激增。西替罗利减少环磷酰胺诱导的小鼠卵巢卵泡破坏[1][2]。

名称

• 中文名: 醋酸西曲瑞克
• 英文名: cetrorelix
• 中文别名: 醋酸西曲瑞克 CETRORELIXACETATE
• 英文别名: N-Acetyl-3-(2-naphthyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridinyl)-D-alanyl-L-seryl-L-tyrosyl-N-carbamoyl-D-ornithyl-L-leucyl-L-arginyl-L-prolyl-D-alaninamide; CETRORELIX ACETATE(CETROTIDE); N-Acetyl-3-(2-naphthalenyl)-D-Ala-4-chloro-D-Phe-3-(3-pyridyl)-D-Ala-L-Ser-L-Tyr-N5-(aminocarbonyl)-D-Orn-L-Leu-L-Arg-L-Pro-D-Ala-NH2; Cetrorelixum [inn-latin]; (2S)-N-[(2R)-1-Amino-1-oxopropan-2-yl]-1-[(2S,5S,8R,11S,14S,17R,20R,23R)-2-(3-carbamimidamidopropyl)-8-[3-(carbamoylamino)propyl]-20-(4-chlorobenzyl)-11-(4-hydroxybenzyl)-14-(hydroxymethyl)-5-isobutyl-23-(2-naphthylmethyl)-4,7,10,13,16,19,22,25-octaoxo-17-(pyridin-3-ylmethyl)-3,6,9,12,15,18,21,24-octaazahexacosan-1-oyl]pyrrolidine-2-carboxamide (non-preferred name); Ac-DNal-DpCl-Phe-DPal-Ser-Tyr-DCit-Leu-Arg-Pro-D-Ala-NH2; N-Acetyl-3-(2-naphthalenyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridinyl)-D-alanyl-L-seryl-L-tyrosyl-N5-(aminocarbonyl)-D-ornithyl-L-leucyl-L-arginyl-L-prolyl-D-alaninamide; Cetrorelixacetate; Ac-D-Nal-D-Cpa-D-Pal-Ser-Tyr-D-Cit-Leu-Arg-Pro-D-Ala-NH2; AC-(D-ALA[3-(2-NAPHTHYL)])-[D-PHE(4-CL)]-(D-ALA[3-(3-PYRIDYL)])-SER-TYR-(D-CIT)-LEU-ARG-PRO-D-ALA-OH; Cetrorelixum; cetrorelixum [INN_la]; CETRORELIX ACID; D-Alaninamide, N-acetyl-3-(2-naphthalenyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridinyl)-D-alanyl-L-seryl-L-tyrosyl-N-(aminocarbonyl)-D-ornithyl-L-leucyl-L-arginyl-L-prolyl-; Unii-oon1hfz4ba; CETRIZINEDIHYDROCHLORIDE; Cetrorelix acetate; N-Acetyl-3-(2-naphthyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(pyridin-3-yl)-D-alanyl-L-seryl-L-tyrosyl-N-carbamoyl-D-ornithyl-L-leucyl-L-arginyl-L-prolyl-D-alaninamide; AC-D-2-NAL-4-CHLORO-D-PHE-B-(3-PYRIDYL)-D-ALA-SER-TYR-D-CIT-LEU-ARG-PRO-D-ALA-NH2; Cetrorelix

物化性质

• 密度: 1.4±0.1 g/cm3
• 分子式: C₇₀H₉₂ClN₁₇O₁₄
• 分子量: 1431.038
• 精确质量: 1429.669800
• PSA: 495.67000
• LogP: 2.69
• 外观性状: 白色粉末
• 折射率: 1.668
• 储存条件: 2-8°C

生物活性

• 描述: 西曲利是一种有效的促性腺激素释放激素(GnRH)拮抗剂。西曲利抑制卵巢刺激期间内源性黄体生成激素激增。西替罗利减少环磷酰胺诱导的小鼠卵巢卵泡破坏[1][2]。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> GNRH受体
  研究领域 >> 内分泌
• 参考文献:

  [1]. Diedrich K, et al. Suppression of the endogenous luteinizing hormone surge by the gonadotrophin-releasing hormone antagonist Cetrorelix during ovarian stimulation. Hum Reprod. 1994 May;9(5):788-91.

  [2]. Meirow D, et al. The GnRH antagonist cetrorelix reduces cyclophosphamide-induced ovarian follicular destruction in mice. Hum Reprod. 2004 Jun;19(6):1294-9.

合成路线

15761-39-4 13139-15-6 3744-87-4 13836-37-8 ~% 详细

文献：Journal of medicinal chemistry, , vol. 36, # 7 p. 928 - 933

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