54784-44-0

• 常用中文名：GLP-DPHE-TRP-SER-TYR-DALA-LEU-ARG-PRO-GLY-NH2: GLP-DF-WSY-DA-LRPG-NH2
• 常用英文名：a d lh-rh
• CAS号：54784-44-0
• 分子式：C₅₉H₇₉N₁₅O₁₃
• 分子量：1206.35000
• 相关类别： 研究领域 内分泌
• 发布时间：2018-12-29 22:47:32
• 更新时间：2024-04-05 14:50:36
• [D-Phe2,D-Ala6]-LH-RH是一种有效的LH-RH拮抗剂。[D-Phe2,D-Ala6]-LH-RH具有抗LH/FSH-RH和抗排卵活性[1]。

名称

• 中文名: GLP-DPHE-TRP-SER-TYR-DALA-LEU-ARG-PRO-GLY-NH2: GLP-DF-WSY-DA-LRPG-NH2
• 英文名: a d lh-rh
• 英文别名: GLP-DPHE-TRP-SER-TYR-DALA-LEU-ARG-PRO-GLY-NH2; [D-PHE2,D-ALA6]-LH-RH (HUMAN); PYR-D-PHE-TRP-SER-TYR-D-ALA-LEU-ARG-PRO-GLY-NH2; [D-PHE2,D-ALA6]-LH-RH; PGLU-D-PHE-TRP-SER-TYR-D-ALA-LEU-ARG-PRO-GLY-NH2; D-phe2,D-ala6-luteinizing hormone*releasing hormo; wy-18,185; LHRH,Phe(2)-Ala(6); (d-phe(sup2))-(d-ala(sup6))-lhrh

物化性质

• 密度: 1.46g/cm3
• 分子式: C₅₉H₇₉N₁₅O₁₃
• 分子量: 1206.35000
• 精确质量: 1205.60000
• PSA: 443.45000
• LogP: 2.77280
• 折射率: 1.687

生物活性

• 描述: [D-Phe2,D-Ala6]-LH-RH是一种有效的LH-RH拮抗剂。[D-Phe2,D-Ala6]-LH-RH具有抗LH/FSH-RH和抗排卵活性[1]。
• 相关类别:
  研究领域 >> 内分泌
  信号通路 >> 其他 >> 其他
• 体内研究: [D-Phe2,D-Ala6]-LH-RH抑制未成年雄性大鼠中LH-RH诱导的LH和FSH释放[1]。[D-Phe2,D-Ala6]-LH-RH(1 mg/大鼠,SC)显示出显著的抗排卵和避孕活性[2]。[D-Phe2,D-Ala6]-LH-RH(0.625,1.25,2.5 mg/kg；皮下注射；单剂量；处死30分钟)导致25日龄垂体切除(低氧)大鼠的茎秆中隆起(SME)-LHRH活性呈剂量依赖性增加,并降低血浆LHRH活性[3]。[D-Phe2,D-Ala6]-LH-RH(25 mg/kg；皮下注射；单剂量)可有效阻断LRH单独诱导的排卵[4]。动物模型：成年雌性Sprague-Dawley大鼠(200-250 g)[2]剂量：1 mg/大鼠给药：SC注射,发情前12:00至14:30小时结果：显示出显著的抗排卵和避孕活性,排卵抑制率为96%。
• 参考文献:

  [1]. Vilchez-Martinez JA, et al. Comparison of the anti-LH/FSH-RH and anti-ovulatory activities of (D-Phe2, D-Leu6)-LH-RH and (D-Phe2, D-Ala6)-LH-RH. Endocr Res Commun. 1976;3(3-4):231-41.

  [2]. Beattie CW, et al. Luteinizing hormone-releasing hormone. Antiovulatory activity of analogs substituted in positions 2 and 6. J Med Chem. 1975 Dec;18(12):1247-50.

  [3]. Corbin A, et al. Effect of luteinizing hormone releasing hormone (LHRH) and an LHRH antagonist of hypothalamic and plasma LHRH of hypophysectomized rats. Endocrinology. 1976 Jan;98(1):247-50.

  [4]. Corbin A, et al. Ihibition of the pre-ovulatory proestrous gonadotropin surge, ovulation and pregnancy with a peptide analogue of luteinizing hormone releasing hormone. Endocr Res Commun. 1975;2(1):1-23.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : OK6600000 CHEMICAL NAME : Luteinizing hormone-releasing hormone, (D-phe(sup 2))-(D-ala(sup 6))- CAS REGISTRY NUMBER : 54784-44-0 LAST UPDATED : 198910 DATA ITEMS CITED : 4 MOLECULAR FORMULA : C59-H79-N15-O13 MOLECULAR WEIGHT : 1206.53 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 3750 ug/kg SEX/DURATION : female 1 day(s) pre-mating TOXIC EFFECTS : Reproductive - Fertility - other measures of fertility REFERENCE : JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 18,1247,1975 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 2500 ug/kg SEX/DURATION : female 1 day(s) pre-mating TOXIC EFFECTS : Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated) REFERENCE : IJGOAL International Journal of Gynaecology & Obstetrics. (Elsevier Scientific Pub. Ireland Ltd., POB 85, Limerick, Ireland) V.7- 1969- Volume(issue)/page/year: 16,359,1979 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intramuscular DOSE : 30 mg/kg SEX/DURATION : female 1 day(s) pre-mating TOXIC EFFECTS : Reproductive - Fertility - other measures of fertility REFERENCE : EDRCAM Endocrine Research Communcations. (New York, NY) V.1-9, 1974-83. Volume(issue)/page/year: 2,1,1975 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 12500 ug/kg SEX/DURATION : female 1 day(s) pre-mating TOXIC EFFECTS : Reproductive - Fertility - other measures of fertility REFERENCE : EDRCAM Endocrine Research Communcations. (New York, NY) V.1-9, 1974-83. Volume(issue)/page/year: 2,1,1975

安全

• 风险声明 (欧洲): 60
• 安全声明 (欧洲): 53-22-36/37/39-45