57773-65-6

• 常用中文名：德舍瑞林
• 常用英文名：Deslorelin
• CAS号：57773-65-6
• 分子式：C₆₄H₈₃N₁₇O₁₂
• 分子量：1282.450
• 相关类别： 生物化工 多肽
• 发布时间：2018-04-02 08:00:00
• 更新时间：2024-01-01 19:55:43
• Deslorelin是GnRH的激动剂。

名称

• 中文名: 地洛瑞林
• 英文名: Deslorelin
• 中文别名: 醋酸德舍瑞林; 德舍瑞林
• 英文别名: Deslorelin; deslorelin acetate; (D-trp6-pro9-NEt)-Gonadotropin Releasing Hormone; Bachem 9022; 5-Oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-tryptophyl-L-leucyl-L-arginyl-N-ethyl-L-prolinamide; [des-Gly10, D-Trp6]-LH-RH ethylamide; MFCD00167401; D-Trp6-pro9-N-ethylamide-LHRH; 6-D-Tryptophan-9-(N-ethyl-L-prolinamide)-10-deglycinamide Luteinizing Hormone-releasing Factor (pig); tryptal; Delorelin acetate; DESORELIN; bachem9022; L-Prolinamide, 5-oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-tryptophyl-L-leucyl-L-arginyl-N-ethyl-; mide)-10-deglycinamide; somagard

物化性质

• 密度: 1.5±0.1 g/cm3
• 沸点: 1783.4ºC at 760 mmHg
• 分子式: C₆₄H₈₃N₁₇O₁₂
• 分子量: 1282.450
• 闪点: 1032.4ºC
• 精确质量: 1281.640747
• PSA: 444.83000
• LogP: 0.77
• 外观性状: 白色粉末或近乎于白色粉末
• 折射率: 1.710
• 储存条件: −20°C

生物活性

• 描述: Deslorelin是GnRH的激动剂。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> GNRH受体
  多肽产品
  研究领域 >> 其他
• 参考文献:

  [1]. Lucas X. Clinical use of deslorelin (GnRH agonist) in companion animals: a review. Reprod Domest Anim. 2014 Oct;

  [2]. Bujok J et al. Influence of ovariohysterectomy and deslorelin acetate on the spontaneous activity of the rabbit urinary bladder in vitro. Theriogenology. 2016 Feb;85(3):441-6.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : OK6755000 CHEMICAL NAME : Luteinizing hormone-releasing factor (pig), 6-D-tryptophan-9-(N-ethyl-L-prolinamide)-10- deglycinamide- CAS REGISTRY NUMBER : 57773-65-6 LAST UPDATED : 199706 DATA ITEMS CITED : 13 MOLECULAR FORMULA : C64-H83-N17-O12 MOLECULAR WEIGHT : 1282.64 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 30 ug/kg SEX/DURATION : male 42 day(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count) Reproductive - Paternal Effects - impotence Reproductive - Paternal Effects - other effects on male REFERENCE : NEJMAG New England Journal of Medicine. (Massachusetts Medical Soc., 10 Shattuck St., Boston, MA 02115) V.198- 1928- Volume(issue)/page/year: 305,663,1981 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 1 ug/kg SEX/DURATION : female 1 day(s) pre-mating TOXIC EFFECTS : Reproductive - Maternal Effects - other effects Reproductive - Fertility - other measures of fertility REFERENCE : AJOGAH American Journal of Obstetrics and Gynecology. (C.V. Mosby Co., 11830 Westline Industrial Dr., St. Louis, MO 63146) V.1- 1920- Volume(issue)/page/year: 135,759,1979 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 1 ug/kg SEX/DURATION : female 1 day(s) pre-mating TOXIC EFFECTS : Reproductive - Maternal Effects - other effects Reproductive - Fertility - other measures of fertility REFERENCE : FESTAS Fertility and Sterility. (American Fertility Soc., 608 13th Ave. S, Birmingham, AL 35282) V.1- 1950- Volume(issue)/page/year: 37,209,1982 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 2 ug/kg SEX/DURATION : female 2 day(s) pre-mating TOXIC EFFECTS : Reproductive - Maternal Effects - menstrual cycle changes or disorders Reproductive - Fertility - other measures of fertility REFERENCE : SCIEAS Science. (American Assoc. for the Advancement of Science, 1333 H St., NW, Washington, DC 20005) V.1- 1895- Volume(issue)/page/year: 205,408,1979 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 28 ng/kg SEX/DURATION : male 7 day(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland, accessory glands REFERENCE : ENDOAO Endocrinology (Baltimore). (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21203) V.1- 1917- Volume(issue)/page/year: 105,1191,1979 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 40 ug/kg SEX/DURATION : male 9 day(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - other effects on male Endocrine - changes in luteinizing hormone Endocrine - androgenic REFERENCE : CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1- 1970- Volume(issue)/page/year: 35,79,1987 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 70 ug/kg SEX/DURATION : female 1-7 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated) 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: 26,1545,1983 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 25 ug/kg SEX/DURATION : female 8-12 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - other measures of fertility REFERENCE : ENDOAO Endocrinology (Baltimore). (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21203) V.1- 1917- Volume(issue)/page/year: 110,347,1982 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 35 ug/kg SEX/DURATION : female 1-7 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) REFERENCE : ENDOAO Endocrinology (Baltimore). (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21203) V.1- 1917- Volume(issue)/page/year: 103,2299,1978 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 15 ug/kg SEX/DURATION : female 5-7 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Newborn - live birth index (measured after birth) REFERENCE : ENDOAO Endocrinology (Baltimore). (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21203) V.1- 1917- Volume(issue)/page/year: 103,2299,1978 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Unreported DOSE : 25 ug/kg SEX/DURATION : male 1 day(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count) Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland, accessory glands REFERENCE : 44LVAU "Peptides' Structure and Biological Function, Proceedings of the American Peptide Symposium, 6th, 1979," Cross, E. and J. Meienhofer, eds., Rockford, IL, Pierce Chemical Co., 1979 Volume(issue)/page/year: 6,781,1979 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Implant DOSE : 150 ug/kg SEX/DURATION : female 75 day(s) pre-mating TOXIC EFFECTS : Reproductive - Maternal Effects - menstrual cycle changes or disorders REFERENCE : INJFA3 International Journal of Fertility. (Allen Press, 1041 New Hampshire, St., Lawrence, KS 66044) V.1- 1955- Volume(issue)/page/year: 25,171,1980

安全

• 危害码 (欧洲): T: Toxic;
• 风险声明 (欧洲): R60
• 安全声明 (欧洲): 53-22-36/37/39-45
• WGK德国: 3
• RTECS号: OK6755000

制备

【方法一】
以相应的保护氨基酸单体为原料，通过固相或液相合成法合成制得。