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Fingolimod (hydrochloride)是ISP-1(肉豆蔻素)的衍生物,ISP-1是中草藥辛氏菌的真菌代謝產(chǎn)物,也是鞘氨醇的結(jié)構(gòu)類似物。它是一種新的免疫調(diào)節(jié)劑,通過抑制淋巴細(xì)胞從淋巴器官遷移來延長許多模型中同種異體移植物的存活時(shí)間。Fingolimod (hydrochloride)被鞘氨醇激酶磷酸化,然后作為四種鞘氨醇-1-磷酸(S1P)受體(S1P1、S1P3、S1P4和S1P5)的有效激動(dòng)劑。Fingolimod (hydrochloride)下調(diào)T和B淋巴細(xì)胞上的S1P1受體會(huì)導(dǎo)致這些細(xì)胞從脾臟、淋巴結(jié)、,和Peyer’s貼劑。Fingolimod (hydrochloride)還增強(qiáng)鞘氨醇轉(zhuǎn)運(yùn)蛋白Abcb1和白三烯C4轉(zhuǎn)運(yùn)蛋白Abcc1的活性,并抑制胞漿磷脂酶A2的活性。
艾美捷Fingolimod (hydrochloride):
正式名稱:2-氨基-2-[2-(4-辛基苯基)乙基]-1,3-丙二醇鹽酸鹽
化學(xué)文摘社編號(hào):162359-56-0
同義詞:FTY720
分子式:C19H33NO2 ? HCl
配方重量:343.9
純度:≥98%
配方:(要求更改配方)結(jié)晶固體
溶解度:(了解溶解度方差)
二甲基苯醚: 20 毫克/毫升
二甲基二甲基硫磺酸: 20 毫克/毫升
乙醇:20毫克/毫升
乙醇:PBS (pH 7.2) (1:1): .2 毫克/毫升
存儲(chǔ):-20°C
穩(wěn)定性:≥ 4年
Fingolimod (hydrochloride)參考文獻(xiàn):
1. Brinkmann, V., Pinschewer, D.D., Feng, L., et al. FTY720: Altered lymphocyte traffic results in allograft protection. Transplantation 72(5), 764-769 (2001).
2. Brinkmann, V., Davis, M.D., Heise, C.E., et al. The immune modulator FTY720 targets sphingosine 1-phosphate receptors. J. Biol. Chem. 277(24), 21453-21457 (2002).
3. Matloubian, M., Lo, C.G., Cinamon, G., et al. Lymphocyte egress from thymus and peripheral lymphoid organs is dependent on S1P receptor 1. Nature 427(6972), 355-360 (2004).
4. Honig, S.M., Fu, S., Mao, X., et al. FTY720 stimulates multidrug transporter- and cysteinyl leukotriene-dependent T cell chemotaxis to lymph nodes. J. Clin. Invest. 111(5), 627-637 (2003).
5. Payne, S.G., Oskeritizian, C.A., Griffiths, R., et al. The immunosuppressant drug FTY720 inhibits cytosolic phospholipase A2 independently of sphingosine-1-phosphate receptors. Blood 109(3), 1077-1085 (2007).
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