长川霉素

钙调神经磷酸酶/ PP2B抑制剂。免疫抑制剂和抗真菌活性。

规格或纯度: ≥97.0%

CAS编号: 104987-12-4
分子式: C₄₃H₆₉NO₁₂
分子量: 792.01
EC号: 200-835-2
PubChem编号: 5282071

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货号 (SKU)	包装规格	是否现货
A127632-25mg	25mg	现货
A127632-100mg	100mg	现货
A127632-500mg	500mg	现货
A127632-1g	1g	现货

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基本描述

规格或纯度	≥97.0%
英文名称	Ascomycin
别名	长川霉素；子囊霉素
英文别名	Immunomycin;FK 520;FR 900520;FR-900520;FR900520;FK-520;FK520
生化机理	When we used either CD4+CD8+ thymocytes or peripheral T cells activated by phorbol ester and ionomycin, the cell surface induction of CD5 was also partially blocked by CsA, FK-520 and rapamycin . Ascomycinalso had a 3-fold lower immunosuppressive potency in a popliteal lymph node hyperplasia assay, resulting in an equivalent therapeutic index consistent with a common mechanistic dependence on calcineurin inhibition.Calcineurin/PP2B inhibitor (IC 50 = 49 nM). Forms a FK-506 binding protein 12 (FKBP12) - Ascomycin -Calcineurin complex. Immunosuppressant and antifungal activity in vitro and in vivo .
储存温度	-20°C储存
运输条件	超低温冰袋运输
备注	如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，它们最多可以使用一个月。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。
产品介绍	Ascomycin(Immunomycin, FR-900520, FK520)是tacrolimus (FK506)的类似物，具有很强的免疫抑制剂。A potent immunosuppressive agent Ascomycin(Immunomycin, FR-900520, FK520) is an ethyl analog of tacrolimus (FK506) with strong immunosuppressant properties. A potent immunosuppressive agent application： Ascomycin is a potent immunosuppressive agent that could be used as a potential therapeutic agent for autoimmune diseases. Ascomycin is an inhibitor of PP2. It is an internal standard for LC-MS/MS testing of the immunosuppressants tacrolimus, sirolimus, and everolimus. This Certified Spiking Solution?? is suitable for critical quantitative applications in clinical and diagnostic testing such as therapeutic drug monitoring assays to ensure patients remain within the narrow therapeutic range of these immunosuppressants.

名称和标识符

EC号	200-835-2
IUPAC Name	(1R,9S,12S,13R,14S,17R,18E,21S,23S,24R,25S,27R)-17-ethyl-1,14-dihydroxy-12-[(E)-1-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone
INCHI	InChI=1S/C43H69NO12/c1-10-30-18-24(2)17-25(3)19-36(53-8)39-37(54-9)21-27(5)43(51,56-39)40(48)41(49)44-16-12-11-13-31(44)42(50)55-38(28(6)33(46)23-34(30)47)26(4)20-29-14-15-32(45)35(22-29)52-7/h18,20,25,27-33,35-39,45-46,51H,10-17,19,21-23H2,1-9H3/b24-18+,26-20+/t25-,27+,28+,29-,30+,31-,32+,33-,35+,36-,37-,38+,39+,43+/m0/s1
InChi Key	ZDQSOHOQTUFQEM-NURRSENYSA-N
Canonical SMILES	CCC1C=C(CC(CC(C2C(CC(C(O2)(C(=O)C(=O)N3CCCCC3C(=O)OC(C(C(CC1=O)O)C)C(=CC4CCC(C(C4)OC)O)C)O)C)OC)OC)C)C
分子式	C₄₃H₆₉NO₁₂
关联CAS	11011-38-4
PubChem CID	5282071
分子量	792.01

化学和物理性质

溶解性	Soluble in DMSO (65 mg/ml), ethanol (50 mg/ml), and water (10-50 μM).
沸点	868℃
闪点(℉)	230°F
闪点(℃)	>110℃

安全信息

象形图	Harmful
信号词	Warning
危险声明	H302: Harmful if swallowed H312: Harmful in contact with skin H332: Harmful if inhaled
预防措施声明	P261,P280,P302+P352,P321,P501,P264,P271,P270,P304+P340,P362+P364,P330,P301+P317,P317
WGK Germany	2
RTECS	KD4185000
个人防护装备	dust mask type N95 (US)， Eyeshields， Gloves

参考文献

1. M Kawai,B C Lane,G C Hsieh,K W Mollison,G W Carter,J R Luly. (1993-01-25) Structure-activity profiles of macrolactam immunosuppressant FK-506 analogues.. FEBS letters, 316 ((2)): (107-113). [PMID:7678400]
2. K W Mollison,T A Fey,R A Krause,V A Thomas,A P Mehta,J R Luly. (1993-06-23) Comparison of FK-506, rapamycin, ascomycin, and cyclosporine in mouse models of host-versus-graft disease and heterotopic heart transplantation.. Annals of the New York Academy of Sciences, 685 (): (55-57). [PMID:7689812]
3. Yan P, Nanamori M, Sun M, Zhou C, Cheng N, Li N, Zheng W, Xiao L, Xie X, Ye RD et al.. (2006) The immunosuppressant cyclosporin A antagonizes human formyl peptide receptor through inhibition of cognate ligand binding.. J Immunol, 177 (10): (7050-8). [PMID:17082621]
4. A M Marsland,S Soundararajan,K Joseph,A P Kaplan. (2005-05-19) Effects of calcineurin inhibitors on an in vitro assay for chronic urticaria.. Clinical and experimental allergy : journal of the British Society for Allergy and Clinical Immunology, 35 ((5)): (554-559). [PMID:15898974]
5. J Junker,W Maier,T Lindel,M K?ck. (2005-08-25) Computer-assisted constitutional assignment of large molecules: COCON analysis of ascomycin.. Organic letters, 1 ((5)): (737-740). [PMID:16118875]
6. Daniel B Yarosh,Arely V Pena,Stephanie L Nay,Matthew T Canning,David A Brown. (2005-11-22) Calcineurin inhibitors decrease DNA repair and apoptosis in human keratinocytes following ultraviolet B irradiation.. The Journal of investigative dermatology, 125 ((5)): (1020-1025). [PMID:16297204]
7. John R Carney,Gary W Ashley,Robert L Arslanian,Greg O Buchannan. (2006-02-10) Structure elucidation of new ascomycins produced by genetic engineering.. The Journal of antibiotics, 58 ((11)): (715-721). [PMID:16466025]
8. Kimberly L Napoli. (2006-04-06) Organic solvents compromise performance of internal standard (ascomycin) in proficiency testing of mass spectrometry-based assays for tacrolimus.. Clinical chemistry, 52 ((4)): (765-766). [PMID:16595827]
9. Simone Cristoni,Luigi Rossi Bernardi,Piermario Gerthoux,Paolo Mocarelli,Maura Brambilla,Elisabetta Gonella,Federico Guidugli,Marco Cantu. (2006-07-15) Surface-activated chemical ionization and high-flow gradient chromatography to reduce matrix effect.. Rapid communications in mass spectrometry : RCM, 20 ((16)): (2376-2382). [PMID:16841358]
10. Magdalena Korecka,Sandra G Solari,Leslie M Shaw. (2006-08-04) Sensitive, high throughput HPLC-MS/MS method with on-line sample clean-up for everolimus measurement.. Therapeutic drug monitoring, 28 ((4)): (484-490). [PMID:16885715]
11. K Hoogtanders,J van der Heijden,M Christiaans,P Edelbroek,J P van Hooff,L M L Stolk. (2006-12-23) Therapeutic drug monitoring of tacrolimus with the dried blood spot method.. Journal of pharmaceutical and biomedical analysis, 44 ((3)): (658-664). [PMID:17184953]
12. Nitin S Patil,Rakesh B Mendhe,Ajeet A Sankar,Harish Iyer. (2007-11-03) Procedure for chromatography involving sample solvent with higher elution strength than the mobile phase.. Journal of chromatography. A, 1177 ((2)): (234-242). [PMID:17976633]
13. Nobuo Mochizuki,Etsuko Suka,Kunihiro Matsumoto,Osamu Akimoto,Keiko Ohno,Tsuyoshi Shimamura,Hiroyuki Furukawa,Satoru Todo,Satoshi Kishino. (2008-09-25) Liquid chromatographic method for the determination of sirolimus in blood using electrochemical detection.. Biomedical chromatography : BMC, 23 ((3)): (267-272). [PMID:18814192]
14. Arunima Biswas,Shaeri Mukherjee,Supratik Das,Dennis Shields,Chi Wing Chow,Umadas Maitra. (2010-11-19) Opposing action of casein kinase 1 and calcineurin in nucleo-cytoplasmic shuttling of mammalian translation initiation factor eIF6.. The Journal of biological chemistry, 286 ((4)): (3129-3138). [PMID:21084295]
15. Jennifer N Andexer,Steven G Kendrew,Mohammad Nur-e-Alam,Orestis Lazos,Teresa A Foster,Anna-Sophie Zimmermann,Tony D Warneck,Dipen Suthar,Nigel J Coates,Frank E Koehn,Jerauld S Skotnicki,Guy T Carter,Matthew A Gregory,Christine J Martin,Steven J Moss,Peter F Leadlay,Barrie Wilkinson. (2011-03-09) Biosynthesis of the immunosuppressants FK506, FK520, and rapamycin involves a previously undescribed family of enzymes acting on chorismate.. Proceedings of the National Academy of Sciences of the United States of America, 108 ((12)): (4776-4781). [PMID:21383123]
16. Nariyasu Mano,Marina Nozawa,Mayumi Sato,Masaru Mori,Hiroaki Yamaguchi,Katsuhiro Kanda,Makoto Nogami,Junichi Goto,Miki Shimada. (2011-03-26) Identification and elimination of ion suppression in the quantitative analysis of sirolimus in human blood by LC/ESI-MS/MS.. Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, 879 ((13-14)): (968-974). [PMID:21435955]
17. Murty A R C Bulusu,Karl Baumann,Anton Stuetz. (2011-08-13) Chemistry of the immunomodulatory macrolide ascomycin and related analogues.. Progress in the chemistry of organic natural products, 94 (): (59-126). [PMID:21833838]
18. Engin Yapici,D Rajasekhar Reddy,Lawrence W Miller. (2012-01-25) An adaptable luminescence resonance energy transfer assay for measuring and screening protein-protein interactions and their inhibition.. Chembiochem : a European journal of chemical biology, 13 ((4)): (553-558). [PMID:22271654]
19. Patrizia Ferraboschi,Diego Colombo,Maria De Mieri,Paride Grisenti. (2012-04-19) Evaluation, synthesis and characterization of tacrolimus impurities.. The Journal of antibiotics, 65 ((7)): (349-354). [PMID:22511227]
20. Bernhard F Gibbs,Inna M Yasinska,Luigi Calzolai,Douglas Gilliland,Vadim V Sumbayev. (2014-05-09) Highly specific targeting of human leukocytes using gold nanoparticle-based biologically active conjugates.. Journal of biomedical nanotechnology, 10 ((7)): (1259-1266). [PMID:24804546]
21. Araceli Vázquez-López,Germán Sierra-Paredes,Germán Sierra-Marcu?o. (2006-07-29) Anticonvulsant effect of the calcineurin inhibitor ascomycin on seizures induced by picrotoxin microperfusion in the rat hippocampus.. Pharmacology, biochemistry, and behavior, 84 ((3)): (511-516). [PMID:16872668]
22. Matthew T Canning,Stephanie L Nay,Arely V Pe?a,Daniel B Yarosh. (2006-08-24) Calcineurin inhibitors reduce nuclear localization of transcription factor NFAT in UV-irradiated keratinocytes and reduce DNA repair.. Journal of molecular histology, 37 ((5-7)): (285-291). [PMID:16927198]
23. Germán Sierra-Paredes,Germán Sierra-Marcu?o. (2008-05-17) Ascomycin and FK506: pharmacology and therapeutic potential as anticonvulsants and neuroprotectants.. CNS neuroscience & therapeutics, 14 ((1)): (36-46). [PMID:18482098]
24. Jingjing Xie,Rajiv Thapa,Sergey Reverdatto,David S Burz,Alexander Shekhtman. (2009-05-09) Screening of small molecule interactor library by using in-cell NMR spectroscopy (SMILI-NMR).. Journal of medicinal chemistry, 52 ((11)): (3516-3522). [PMID:19422228]
25. Xiao-ling Qin,Hui-chang Bi,Chang-xi Wang,Jia-li Li,Xue-ding Wang,Long-shan Liu,Xiao Chen,Min Huang. (2009-08-21) Study of the effect of Wuzhi tablet (Schisandra sphenanthera extract) on tacrolimus tissue distribution in rat by liquid chromatography tandem mass spectrometry method.. Biomedical chromatography : BMC, 24 ((4)): (399-405). [PMID:19693766]
26. Jay D Turner,Andrew P Thomas,John P Reeves,Basil M Hantash. (2009-09-18) Calcineurin activation by slow calcium release from intracellular stores suppresses protein kinase C regulation of L-type calcium channels in L6 cells.. Cell calcium, 46 ((4)): (242-247). [PMID:19758695]
27. Jane R Allison,Wilfred F van Gunsteren. (2009-11-03) A method to explore protein side chain conformational variability using experimental data.. Chemphyschem : a European journal of chemical physics and physical chemistry, 10 ((18)): (3213-3228). [PMID:19882615]
28. Heike Burhenne,Jan T Kielstein,Olaf Burkhardt,Volkhard Kaever. (2011-10-25) Quantitative analysis of the antifungal drug anidulafungin by LC-online SPE-MS/MS in human plasma.. Biomedical chromatography : BMC, 26 ((6)): (681-683). [PMID:22020627]

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长川霉素

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基本描述

名称和标识符

化学和物理性质

安全信息

参考文献

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长川霉素

库存信息

库存信息

库存信息

库存信息

基本描述

名称和标识符

化学和物理性质

安全信息

参考文献

相关文档

质检报告COA

产品问答

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