CAS: 74436-00-3; Geclosporin
该化合物是循环性无碳化物,是Cyclosporin A的结构性类似物,具有免疫抑制特性,通过抑制卡列胆素发挥作用,从而抑制T细胞活化和细胞基素生产.与Cyclosporin A, Cyclosporin G相比,它展示了一种独特的药理学特征,包括改变的与环球素的结合和可能减少肾毒性.该化合物主要用于研究免疫抑制机制并探索在自动免疫性疾病和器官移植方面的治疗应用.其结构改变为结构活动关系提供了深刻的见解,有助于开发改良的免疫抑制剂.Cyclospolin G作为实验室使用的高纯度试剂提供,确保实验研究的再生性.
- 英文名称Geclosporin
- 中文名称吉环孢素
- IUPAC名称(3S,6S,9S,12R,15S,18S,21S,24S,30S,33S)-33-((1R,2R,E)-1-hydroxy-2-methylhex-4-en-1-yl)-6,9,18,24-tetraisobutyl-3,21-diisopropyl-1,4,7,10,12,15,19,25,28-nonamethyl-30-propyl-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2,5,8,11,14,17,20,23,26,29,32-undecaone
- 其它别名CyclosporinA, 7-L-norvaline-; 1,4,7,10,13,16,19,22,25,28,31-Undecaazacyclotritriacontane,cyclic peptide deriv.; 7-L-Norvaline cyclosporin A; Cyclo[L-alanyl-D-alanyl-N-methyl-L-leucyl-N-methyl-L-leucyl-N-methyl-L-valyl-(3R,4R,6E)-6,7-didehydro-3-hydroxy-N,4-dimethyl-L-2-amino°Ctanoyl-L-norvalyl-N-methylglycyl-N-methyl-L-leucyl-L-valyl-N-methyl-L-leucyl]; Cyclo[[(2S,3R,4R,6E)-3-hydroxy-4-methyl-2-(methylamino)-6-°Ctenoyl]-L-norvalyl-N-methylglycyl-N-methyl-L-leucyl-L-valyl-N-methyl-L-leucyl-L-alanyl-D-alanyl-N-methyl-L-leucyl-N-methyl-L-leucyl-N-methyl-L-valyl]; Cyclosporine G; Geclosporin
- CAS编号74436-00-3
- MFCD编号:MFCD00867600
- FDA UNII编号:UA3JNW70T9
- 分子式:C63H113N11O12分子量:1216.64
- 产品CID: 1734486
- 相似结构搜索
- 产品信息参考
;;;; - InChIKey: ZMKGDQSIRSGUDJ-XNCHKUNVSA-N
- ZMKGDQSIRSGUDJ-LIAWPGETNA-N
- 计算化学: 氢键受体数12.0氢键供体数5.0可旋转键数16.0
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专利信息
专利号:US-4396542-A
优先权日:1980-02-14
标 题 :Method for the total synthesis of cyclosporins, novel cyclosporins and novel intermediates and methods for their production
发明人：WENGER ROLAND
权利人:SANDOZ LTD
摘要:A method for the total synthesis of cyclosporins, in particular Cyclosporin A, cyclosporins produced in accordance with the method of the invention and novel intermediates, in particular novel [1S, 2R, 3R]- and [1R, 2S, 3S]-1-nitrilo-1-carbonyl-3-methyl-2-oxy-heptanes and -hept-5-enes, employed in the method of the invention.
专利号:US-5214130-A
优先权日:1990-02-27
标题 :Synthesis of novel immunosuppressive cyclosporin analogs with modified amino acids at position-8
发明人：PATCHETT ARTHUR A; TAUB DAVID; GOEGELMAN ROBERT T
权利人:MERCK & CO INC
摘要:New immunosuppressive cyclosporin analogs are disclosed consisting of [dehydro-Ala]8 cyclosporins and derived therefrom cyclosporins having a sulfur containing amino acid at position-8.
专利号:RO-110144-B1
优先权日:1992-02-13
标题 :New cyclosporins, their method of synthesis and method of treatment and prevention of AIDS
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主要参考文献
1: Epting T, Hartmann K, Sandqvist A, Nitschke R, Gordjani N. Cyclosporin A stimulates apical Na+/H+ exchange in LLC-PK1/PKE20 proximal tubular cells. Pediatr Nephrol. 2006 Jul;21(7):939-46. doi: 10.1007/s00467-006-0097-3. Epub 2006 May 11. 27(2):144-50. doi: 10.1097/01.ftd.0000148451.35811.74. 1(9):1466-74. doi: 10.1039/b210086j. 61(2):127-34. 13(6):1406-11. doi: 10.1093/ndt/13.6.1406. 136(9):577-88. 14(10):1466-71. doi: 10.1023/a:1012141309951. 52(4):329-33. French. 37(7):575-86. doi: 10.1002/j.1552-4604.1997.tb04339.x. 10(2):79-84. doi: 10.1159/000211472. 71(7):437-42. doi: 10.1007/s002040050408. 35(3):121-9. doi: 10.1016/1056-8719(96)00022-6. 11(2):277-84. 28(2):892. 51(5):591-8. doi: 10.1016/s0006-2952(95)02175-2. 61(2):355-60. doi: 10.1006/jsre.1996.0129. 18(1):79-87. doi: 10.1016/0192-0561(95)00108-5. 35(12):1136-43. doi: 10.1002/j.1552-4604.1995.tb04038.x. 17(6):655-9. doi: 10.1097/00007691-199512000-00018. 23(5):515-29. doi: 10.1007/BF02353472.
合成参考文献
摘要:Fryer JP, Pascoe EA, Yatscoff RW, Thliveris JA. A comparison of cyclosporine A and cyclosporine G in a rabbit heterotopic cardiac transplant model: graft outcome and histological findings. Histol Histopathol. 1996 Apr;11(2):277–84.
参考文献:10.1007/s00467-006-0097-3
摘要:Epting T, Hartmann K, Sandqvist A, Nitschke R, Gordjani N. Cyclosporin A stimulates apical Na+/H+ exchange in LLC-PK1/PKE20 proximal tubular cells. Pediatr Nephrol. 2006 Jul;21(7):939–46. doi: 10.1007/s00467-006-0097-3.
参考文献:10.1007/bf00372712
摘要:Amsellem C, Haftek M, Kanitakis J, Thivolet J. Effect of cyclosporins A, G, and H on normal and ichthyotic keratinocyte growth in culture. Archives of Dermatological Research. 1992 Jun;284(3):173–8. doi: 10.1007/bf00372712.
参考文献:10.1016/0167-4889(86)90170-9
摘要:Mátyus L, Balázs M, Aszalós A, Mulhern S, Damjanovich S. Cyclosporin A depolarizes cytoplasmic membrane potential and interacts with Ca2+ ionophores. Biochimica et Biophysica Acta (BBA) - Molecular Cell Research. 1986 May;886(3):353–60. doi: 10.1016/0167-4889(86)90170-9.
参考文献:10.1016/0014-2999(93)90666-6
摘要:Mühl H, Kunz D, Rob P, Pfeilschifter J. Cyclosporin derivatives inhibit interleukin 1 beta induction of nitric oxide synthase in renal mesangial cells. Eur J Pharmacol. 1993 Nov 02;249(1):95–100. doi: 10.1016/0014-2999(93)90666-6.
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