CAS: 140703-51-1; Hexarelin
该化合物是一种合成聚醚,可用作生长激素秘密解剖器,主要用于研究环境,刺激从垂垂体腺中释放生长激素.埃卡莫雷林的特点是能够与格列林受体结合,该受体在调控食欲和能量平衡方面起着至关重要的作用.一般通过下皮注射进行,并研究其在治疗生长激素缺陷和其他相关条件方面的潜在应用.其结构由一组氨酸组成,它模拟了格列林的动作,导致内生生长激素水平的上升.埃马列林一般都受到良好的调剂,但和任何一样,它可能具有副作用,包括注射场反应或改变葡萄糖新陈代谢.作为研究化合物,它的使用主要限于临床研究和研究其药理特性和治疗潜力.
- ⚠️《2026年兴奋剂目录》
- 英文名称Hexarelin
- 中文名称艾沙瑞林
- IUPAC名称L-Lysinamide, L-histidyl-2-methyl-D-tryptophyl-L-alanyl-L-tryptophyl-D-phenylalanyl-
- 其它别名L-Histidyl-2-methyl-D-tryptophyl-L-alanyl-L-tryptophyl-D-phenylalanyl-L-lysinamide; Examorelin
- CAS编号140703-51-1
- MFCD编号:MFCD00671439
- FDA UNII编号:09QF37C617
- 分子式:C47H58N12O6
- 分子量:887.04
- 产品CID: 626444
- 产品分类生物化工 → 多肽
- 相似结构搜索
- InChIKey: RVWNMGKSNGWLOL-GIIHNPQRSA-N
- RVWNMGKSNGWLOL-GIIHNPQRSA-N…
- 计算化学: 氢键受体数9.0氢键供体数11.0可旋转键数23.0
物理性质
- 沸点1403.6 °C at 760 mmHg
- 闪点802.7 °C
- 密度1.322 g/cm3
- pKa:13.42±0.46(预测)
- PSA:300.89
- LogP:5.3922
- 折射率1.66
- 蒸汽压0mmHg at 25°C
- 溶解性水: Soluble1mg/mL, Clear, Colorless
- 外观形态结晶性固体
- 储存条件-20°C
- 产品应用该化合物是合成生长激素-解冻(GHRP),刺激从前垂垂垂体分泌生长激尔蒙(GHN),对GHRELIN受体(GHS-R1A)具有约束力,通过启动G蛋白混合受体途径和随后释放内生GHHM的机制触发GG释放.EXAORELIN在临床环境中用于评估生长激ALM分泌,并有可能用于生长激LE缺乏治疗.
合成工艺路线路线简述
海关参考信息
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2912110000-甲醛
2912120000-乙醛
2921211000-乙二胺 - 💡 提示：海关信息按照顺序优先匹配，如需确认的海关信息，请参考相关资料。
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专利信息
专利号:US-9353057-B2
优先权日:2003-12-30
标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
发明人：GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
权利人:XENOPORT INC
摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.
专利号:US-12351573-B2
优先权日:2019-05-09
标 题:Compounds for use in synthesis of peptidomimetics
发明人：AL-ABED YOUSEF; CHENG KAI FAN
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.
专利号:US-2023159450-A1
优先权日:2020-05-08
标 题 :Dimers for use in synthesis of peptidomimetics
发明人：AL-ABED YOUSEF; ALTITI AHMAD
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Dimers for use in synthesis of peptidomimetics are described. Uses of dimers as synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the dimers and uses of azapeptides and other peptidomimetics are also described.
专利号:US-2020354404-A1
优先权日:2019-05-09
标 题 :Peptidomimetic agents, synthesis and uses thereof
发明人：AL-ABED YOUSEF
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.
专利号:US-2015158809-A9
优先权日:2013-02-26
标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
发明人：WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
权利人:XENOPORT INC
摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.
专利号:US-8598153-B2
优先权日:2006-09-22
标题 :Method of treatment using fatty acid synthesis inhibitors
发明人：SINGH SHEO B; TOTA MICHAEL R; WANG JUN
权利人:SINGH SHEO B; TOTA MICHAEL R; WANG JUN; MERCK SHARP & DOHME
摘要:The present invention relates to natural products that possess fatty acid synthesis inhibitor activity and can be used to treat and prevent diseases such as obesity, cancer, diabetes, fungal infections, Mycobacterium tuberculosis infections, malarial infections and other apicomplexan protozoal diseases.
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主要参考文献
1: Mao Y, Tokudome T, Kishimoto I, Otani K, Miyazato M, Kangawa K. One dose of oral hexarelin protects chronic cardiac function after myocardial infarction. Peptides. 2014 Jun;56:156-62. doi: 10.1016/j.peptides.2014.04.004. doi: 10.1210/en.2013-1291. doi: 10.1152/ajpheart.00257.2011. doi: 10.1007/s12020-015-0531-z. Review. doi: 10.11909/j.issn.1671-5411.2014.03.007. Review.
6: Semenistaya E, Zvereva I, Thomas A, Thevis M, Krotov G, Rodchenkov G. Determination of growth hormone releasing peptides metabolites in human urine after nasal administration of GHRP-1, GHRP-2, GHRP-6, Hexarelin, and Ipamorelin. Drug Test Anal. 2015 Oct;7(10):919-25. doi: 10.1002/dta.1787. doi: 10.1016/j.ejphar.2011.08.020. doi: 10.1016/j.peptides.2009.11.007. doi: 10.1016/j.ijpharm.2009.05.057. doi: 10.1371/journal.pone.0149730.
12: Barlind A, Karlsson N, Åberg ND, Björk-Eriksson T, Blomgren K, Isgaard J. The growth hormone secretagogue hexarelin increases cell proliferation in neurogenic regions of the mouse hippocampus. Growth Horm IGF Res. 2010 Feb;20(1):49-54. doi: 10.1016/j.ghir.2009.09.001. doi: 10.1071/RD11009.
合成参考文献
参考文献:10.1007/bf03343574
摘要:Guzzaloni G, Grugni G, Morabito F. Hexarelin-induced growth hormone response in short stature. Comparison with growth hormone-releasing hormone plus pyridostigmine and arginine plus estrogen. Journal of Endocrinological Investigation. 1999 May;22(5):360–8. doi: 10.1007/bf03343574.
参考文献:10.1210/jc.84.7.2489|10.1210/jcem.84.7.5811
摘要:Korbonits M, Kaltsas G, Perry LA, Putignano P, Grossman AB, Besser GM, Trainer PJ. The Growth Hormone Secretagogue Hexarelin Stimulates the Hypothalamo-Pituitary-Adrenal Axis via Arginine Vasopressin. The Journal of Clinical Endocrinology & Metabolism. 1999 Jul;84(7):2489–95. doi: 10.1210/jcem.84.7.5811.
参考文献:10.1016/s1388-9842(01)00223-9
摘要:Imazio M, Bobbio M, Broglio F, Benso A, Podio V, Valetto MR, Bisi G, Ghigo E, Trevi GP. GH-independent cardiotropic activities of hexarelin in patients with severe left ventricular dysfunction due to dilated and ischemic cardiomyopathy. Eur J Heart Fail. 2002 Mar;4(2):185–91. doi: 10.1016/s1388-9842(01)00223-9.
摘要:Newell-Price J, Grossman A. Biochemical and imaging evaluation of Cushing's syndrome. Minerva Endocrinol. 2002 Jun;27(2):95–118.
参考文献:10.1007/bf03041053
摘要:Schmidt A, Fabrizii V, Maier C, Riedl M, Schmidt A, Kotzmann H, Geyer G, Luger A. Normal regulation of elevated plasma ghrelin concentrations in dialysis patients. Wien Klin Wochenschr. 2004 Apr 30;116(7-8):235–9. doi: 10.1007/bf03041053.
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