中文名 | 雷帕霉素 |
英文名 | Sirolimus |
别名 | 雷帕酶素 西罗莫司 雷帕霉素 雷帕霉素D3 依维莫司杂质17 雷帕霉素,来源于吸水链霉菌 雷帕霉素-D3 (雷帕霉素-D3) MTOR抑制剂(RAPAMYCIN) |
英文别名 | RPM RAPA AY 22989 RAPAMUNE RAPAMYCIN Sirolimus Rapamycin Rapammune NSC-226080 (-)-Rapamycin Antibiotic AY 22989 RAPAMYCIN, STREPTOMYCES HYGROSCOPICUS 23,27-EPOXY-3H-PYRIDO(2,1-C)(1,4)OXAAZACYCLOHENTRIACONTINE (3S,6R,7E,9R,10R,12R,14S,15Z,17E,19E,21S,26R,27R,34aS)-9,27-dihydroxy-3-{(1R)-2-[(1S,3R,4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylethyl}-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-9,10,12,13,14,21,22,23,24,25,26,27,32,33,34,34a-hexadecahydro-3H-23,27-epoxypyrido[2,1-c][1,4]oxazacyclohentriacontine-1,5,11,28,29(4H,6H,31H)-pentone (3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,27-dihydroxy-3-{(2R)-1-[(1S,3R,4R)-4-hydroxy-3-methoxycyclohexyl]propan-2-yl}-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-9,10,12,13,14,21,22,23,24,25,26,27,32,33,34,34a-hexadecahydro-3H-23,27-epoxypyrido[2,1-c][1,4]oxazacyclohentriacontine-1,5,11,28,29(4H,6H,31H)-pentone (3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,10,12,13,14,21,22,23,24,25,26,27,32,33,34,34a- Hexadecahydro-9,27-dihydroxy-3-((1R)-2-((1S,3R,4R)-4-hydroxy-3-methoxycyclohexyl)-1-methylethyl)-10,21-imethoxy- 6,8,12,14,20,26-hexamethyl-23,27-epoxy-3H-pyrido(2,1-c)(1,4)oxaazacyclohentriacontine-1,5,11,28,29(4H,6H,31H)-pentone 23,27-Epoxy-3H-pyrido(2,1-c)(1,4)oxaazacyclohentriacontine-1,5,11,28,29(4H,6H,31H)-pentone, 9,10,12,13,14,21,22,23,24,25,26,27,32,33,34,34a-hexadecahydro-9,27-dihydroxy-3-(3-(4-hydroxy-3-methoxycyclohexyl)-1-methylethyl)-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-, (3S-(3R*S*1R*,3S*,4S*)),6S*,7E,9S*,10S*,12S*,14R*,15E,17E,19E,21R*,23R*,26S*,27S*,34aR*))- |
CAS | 53123-88-9 |
EINECS | 610-965-5 |
化学式 | C51H79NO13 |
分子量 | 914.19 |
InChI | InChI=1/C51H79NO13/c1-30-16-12-11-13-17-31(2)42(61-8)28-38-21-19-36(7)51(60,65-38)48(57)49(58)52-23-15-14-18-39(52)50(59)64-43(33(4)26-37-20-22-40(53)44(27-37)62-9)29-41(54)32(3)25-35(6)46(56)47(63-10)45(55)34(5)24-30/h11-13,16-17,25,30,32-34,36-40,42-44,46-47,53,56,60H,14-15,18-24,26-29H2,1-10H3/b13-11+,16-12-,31-17+,35-25+/t30-,32-,33-,34-,36-,37+,38?,39+,40-,42+,43+,44-,46-,47+,51-/m1/s1 |
密度 | 1.0352 (rough estimate) |
熔点 | 183-185°C |
沸点 | 799.83°C (rough estimate) |
比旋光度 | D25 -58.2° (methanol) |
闪点 | 87 °C |
水溶性 | Soluble in DMSO at 50mg/ml or methanol at 25mg/mlSoluble in alcohol, dimethyl sulfoxide and dimethyl formamide. Insoluble in water. |
蒸汽压 | 0.56 hPa ( 20 °C) |
溶解度 | 乙醇: 可溶2mm |
折射率 | 1.5280 (estimate) |
酸度系数 | 10.40±0.70(Predicted) |
存储条件 | -20°C |
稳定性 | 稳定2年?从提供的购买日期开始。?DMSO或乙醇中的溶液可以在-20 °C下储存长达2个月。 |
敏感性 | Moisture Sensitive/Light Sensitive/Hygroscopic |
外观 | 溶液 |
颜色 | colorless to yellow |
Merck | 14,8114 |
MDL号 | MFCD00867594 |
危险品标志 | Xi - 刺激性物品 Xn - 有害物品 F - 易燃物品 |
风险术语 | R36/38 - 刺激眼睛和皮肤。 R36 - 刺激眼睛。 R20/21/22 - 吸入、皮肤接触及吞食有害。 R11 - 高度易燃。 |
安全术语 | S22 - 切勿吸入粉尘。 S24/25 - 避免与皮肤和眼睛接触。 S37/39 - 戴适当的手套和护目镜或面具。 S26 - 不慎与眼睛接触后,请立即用大量清水冲洗并征求医生意见。 S36/37 - 穿戴适当的防护服和手套。 S16 - 远离火源。 |
危险品运输编号 | UN 1648 3 / PGII |
WGK Germany | 2 |
RTECS | VE6250000 |
海关编号 | 29349990 |
下游产品 | 甲基磷酸乙酯 159351-68-5 |
参考资料 展开查看 | 1. 李竹英,田春燕,蒋鹏娜,马建.基于PI3K/Akt/mTOR信号通路探讨平喘颗粒对气道上皮细胞自噬的作用机制[J].中华中医药杂志,2019,34(11):5094-5098. 2. 陆树萍, 丁红生. 红景天苷经自噬途径减少脑出血后继发神经损伤的的机制探讨[J]. 中华中医药学刊, 2019(4). 3. 郭娟, 张迪, 李龙,等. 细胞自噬对犬骨髓间充质干细胞干性的影响[J]. 畜牧兽医学报, 2020, v.51(02):166-174. 4. 蔡旭华,朱伟华,李伟平.西罗莫司对非酒精性脂肪肝大鼠调节性T细胞/辅助性T细胞17平衡的影响[J].中国临床药理学杂志,2017,33(01):36-39. 5. 单冬炜,经涛,沈建华,丁冬官,祝兵,谢平,于惠敏.雷帕霉素在视网膜母细胞瘤婴幼儿患者中的应用及对预后的影响[J].肿瘤药学,2017,7(05):605-609. 6. 刘波, 陈澍, 杜心灵,等. 雷帕霉素降低炎症因子表达水平对小鼠心肌梗死的影响[J]. 华中科技大学学报:医学版, 2013, 42(4):391-391. 7. 饶春梅 成细华 任婷 孙彦波 彭霞 黄政德.加味丹参饮含药血清对缺氧/复氧H9C2心肌细胞自噬相关蛋白LC3Ⅱ及Beclin1表达的影响[J].中医杂志 2017 58(12):1043-1048. 8. 饶春梅 成细华 任婷 孙彦波 彭霞 黄政德.加味丹参饮含药血清预处理对缺氧/复氧H9C2心肌细胞自噬相关基因Atg5和Beclin1 mRNA表达的影响[J].中国老年学杂志 2017 37(08):1821-1824. 9. 蒋鹏娜,王丽洁,李星,李竹英.平喘颗粒对气道上皮细胞自噬及凋亡的抑制作用探讨[J].中国中医急症,2020,29(11):1902-1905. 10. 朱鸷翔,沈松鹤,赵森,王大勇,王志学,李荟苹.腹主动脉灌注雷帕霉素联合肝动脉化疗治疗肝移植瘤兔模型疗效分析[J].现代肿瘤医学,2020,28(23):4032-4036. 11. Li, Cuijie, et al. "Long noncoding RNA H19 act as a competing endogenous RNA of Let‐7g to facilitate IEC‐6 cell migration and proliferation via regulating EGF." Journal of cellular physiology 236.4 (2021): 2881-2892.https://doi.org/10.1002/jcp.30061 12. Li, Cuijie, et al. "Epidermal growth factor regulation by autophagy‐mediated lncRNA H19 in murine intestinal tract after severe burn." Journal of cellular and molecular medicine 24.10 (2020): 5878-5887.https://doi.org/10.1111/jcmm.15262 13. Xinghui Song, Jinglin Gao, Huicong Liu, Xiuhua Liu, Kaijiang Tang, Rapamycin alleviates renal damage in mice with systemic lupus erythematosus through improving immune response and function, Biomedicine & Pharmacotherapy, Volume 137, 2021, 111289, ISSN 075 14. [IF=3.476] Duanyang Zhang et al."Autophagy can alleviate severe burn-induced damage to the intestinal tract in mice."Surgery. 2017 Aug;162:408 15. [IF=6.529] Xinghui Song et al."Rapamycin alleviates renal damage in mice with systemic lupus erythematosus through improving immune response and function."Biomed Pharmacother. 2021 May;137:111289 16. [IF=5.959] Pan Haitao et al."Autophagic flux disruption contributes to Ganoderma lucidum polysaccharide-induced apoptosis in human colorectal cancer cells via MAPK/ERK activation."Cell Death Dis. 2019 Jun;10(6):1-18 17. [IF=5.546] Cuijie Li et al."Long noncoding RNA H19 act as a competing endogenous RNA of Let‐7g to facilitate IEC‐6 cell migration and proliferation via regulating EGF."J Cell Physiol. 2021 Apr;236(4):2881-2892 18. [IF=5.34] Guanghong Chen et al."Myricetin suppresses the proliferation and migration of vascular smooth muscle cells and inhibits neointimal hyperplasia via suppressing TGFBR1 signaling pathways."Phytomedicine. 2021 Nov;92:153719 19. [IF=5.192] Chunliu Mi et al."Digitoxin promotes apoptosis and inhibits proliferation and migration by reducing HIF-1α and STAT3 in KRAS mutant human colon cancer cells."Chem-Biol Interact. 2022 Jan;351:109729 20. [IF=4.486] Cuijie Li et al."Epidermal growth factor regulation by autophagy‐mediated lncRNA H19 in murine intestinal tract after severe burn."J Cell Mol Med. 2020 May;24(10):5878-5887 21. [IF=1.892] Weiwei Zhao et al."High pathogenicity island is associated with enhanced autophagy in pathogenic Escherichia coli HPI - infected macrophages."Res Vet Sci. 2021 Mar;135:113 22. [IF=4.677] Wang Hao et al."mTOR deletion ameliorates CD4 + T cell apoptosis during sepsis by improving autophagosome-lysosome fusion."APOPTOSIS. 2022 Apr;:1-8 23. [IF=6.543] Gong Wan et al."Orcinol Glucoside Improves Senile Osteoporosis through Attenuating Oxidative Stress and Autophagy of Osteoclast via Activating Nrf2/Keap1 and mTOR Signaling Pathway."Oxidative Medicine and Cellular Longevity. 2022;2022:5410377 |
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