- SKI II
- PF-543
- Ozanimod (RPC1063)
- BAF312 (Siponimod)
| Fingolimod (FTY720)S1P receptors agonist |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
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- Purity = 99.42%
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Chemical structure
| Description | Fingolimod is a mechanistically novel, orally bioavailable therapy for multiple sclerosis (MS). | |||||
| Targets | S1P1 | S1P3 | S1P4 | S1P5 | ||
| IC50 | ||||||
| Cell experiment: [1] | |
Cell lines | MCF-7, MDA-MB-231, Sk-Br-3, HCT-116 and SW620 cells |
Preparation method | The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
Reaction Conditions | IC50: 79.1 μM (MCF-7), 59.9 μM (MDA-MB-231), 72.9 μM (Sk-Br-3), > 100 μM (HCT-116) and 40.0 μM (SW620); 48 hours |
Applications | The IC50 values of fingolimod were determined by a WST-1 assay. The results demonstrated that treatment of the compound caused cell death in a dose-dependent manner. Fingolimod exhibited comparatively low IC50 values within the concentration range of 5-7μM for all of the cells tested in this study. |
| Animal experiment: [2] | |
Animal models | C57BL/6J mice |
Dosage form | Intraperitoneal injection, 0.1 mg per kg of body weight |
Applications | As early as 30 min after injection of fingolimod (0.1 mg per kg of body weight), the levels of phosphorylated ERK1/2 (pERK1/2) were significantly increased in hippocampal neurons. After an additional 30 min, BDNF mRNA levels were elevated, and protein levels were significantly increased in the hippocampus, the cortex, and the striatum after 48 h. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1] Nagaoka Y, Otsuki K, Fujita T, et al. Effects of phosphorylation of immunomodulatory agent FTY720 (fingolimod) on antiproliferative activity against breast and colon cancer cells. Biological and Pharmaceutical Bulletin, 2008, 31(6): 1177-1181. [2] Deogracias R, Yazdani M, Dekkers M P J, et al. Fingolimod, a sphingosine-1 phosphate receptor modulator, increases BDNF levels and improves symptoms of a mouse model of Rett syndrome. Proceedings of the National Academy of Sciences, 2012, 109(35): 14230-14235. | |
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| Cas No. | 162359-56-0 | SDF | Download SDF |
| Synonyms | Gilenia; FTY 720;FTY-720 | ||
| Chemical Name | 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol;hydrochloride | ||
| Canonical SMILES | CCCCCCCCC1=CC=C(C=C1)CCC(CO)(CO)N.Cl | ||
| Formula | C19H34ClNO2 | M.Wt | 343.94 |
| Solubility | ≥17.2mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Fingolimod is a mechanistically novel, orally bioavailable therapy for multiple sclerosis (MS) [1].
Fingolimod is a FDA approved drug for Multiple sclerosis treatment. It is a folk medicine emerged from Fungi. Fingolimod was firstly found to be a therapeutic agent in organ transplantation. Then Fingolimod was found to have similar structure with natural sphingosine and interact with S1P1, S1P4, S1P5 and S1P3 receptors as high affinity agonist with EC50 values of 0.3-3.1 nM. It plays the role in MS treatment through receptor-mediated actions both on the immune system and in the CNS. Fingolimod can prevent normal lymphocyte egress and reduce the infiltration of autoaggressive lymphocytes into the CNS [1, 2].
References:[1] Chun J, Brinkmann V. A mechanistically novel, first oral therapy for multiple sclerosis: the development of fingolimod (FTY720, Gilenya). Discovery medicine, 2011, 12(64): 213.[2] Chun J, Hartung H P. Mechanism of action of oral fingolimod (FTY720) in multiple sclerosis. Clinical neuropharmacology, 2010, 33(2): 91.
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小弟有一中药处方，需要水煮醇沉处理，问下具体该怎么做，给我方子的老师去世了
告诉我中药先水煮，在用水煮醇沉法外敷治疗
给电话我直接问液可以
各位老师好,有做环黄芪醇的吗?其对心血管效果怎么样?使用剂量范围是不是很窄,我看文献,有报道,黄芪提取物对血管的作有是双向的,会不会在低剂量时对身体是有害的
完全醇水溶液如长期存放，会出现粘度增加甚至凝胶化的现象，聚合度和粘度越高，储存温度越低，越容易出现这种想象。可以采取以下措施：
（1）将聚乙烯醇水溶液重新加热搅拌即可恢复原来的流动性。
（2）添加硫氰盐酸盐（如钙、钠、铵等盐类）、苯酚、丁醇、山梨酸等可以有效防止凝胶化，添加量为5~10%。部分醇解型PVA长期存放不易产生粘度增加的情况。同时要注意长期存放容易发生发霉、腐化现象，需添加防霉、防腐剂。建议配置好水溶液后即时使用。
在本例中，溴处在间位，因此不参与反应。
而氯恰好处于对位，因而能发生反应，被甲氧基取代。
因此产物是4-硝基-2-溴苯甲醚。
各位亲，本人用70%乙醇回流提了中药大概70L，准备旋蒸浓缩但一直没浓缩，室温放了5天，之后要做药理试验的，会不会影响药效？需要重提吗？感谢感谢
（二）连接回流冷凝管时，冷凝管连接水不会对浸出物造成影响吗？
请求大神指点，不胜感激！
本人目前在做一个中药提取方法的研究，水提醇沉，醇沉浓度分别为50%、60%和70%,检验结果，得率分别为21.99%、23.85%和25.55%，但含量分别是33.48mg/g、16.60mg/g和19.42mg/g。理论上是醇沉浓度越高，去除的杂质越多，得率越低吗？含量是不是也应该是醇沉浓度越高含量越高？我的试验有什么问题，求各位大虾指点！
我想提取中药中的有效成分，好像目前醇提取的比较多，中药有比如黄柏，桑白皮这些。有谁知道醇提取步骤吗？能不能帮帮忙，万分感激
补充：
一般使用浓硫酸作催化剂，使醇类脱去羟基生成含双键的有机物。应注意的是醇发生消去反应时的温度控制，温度较低(140℃)时会生成副产物醚类，温度达到一定范围（170℃）时才会发生消去反应。消去反应的本质是羟基与β位上的一个H原子共同脱去生成H2O的反应，因而能发生消去反应的醇类必须要有β-H原子。
如果羟基相连接的碳的邻位碳有多个，且都有氢原子，则消去有氢原子较少的邻位碳上的氢原子。 示例：
乙醇发生消去反应的方程式
CH3CH2OH→CH2=CH2+H2O （条件为浓硫酸 170摄氏度）
求助战友们：
有做过中药醇提取，但是在收醇的时候，当浓缩至醇浓度约20%的时候，有析出现象，析出的还是我的有效成分，怎么才能解决这个问题呢？如果在未析出时停止浓缩，药液太稀，无法干燥呢？
问题1：我该如何浓缩定参数？
问题2：如果在未析出时放液，由于药液太稀，我该如何选择干燥方式？
求助站里的大侠们，谢谢！
