Fingolimod (hydrochloride):一種新型免疫調(diào)節(jié)劑
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)的有效激動劑。Fingolimod (hydrochloride)下調(diào)T和B淋巴細胞上的S1P1受體會導(dǎo)致這些細胞從脾臟、淋巴結(jié)、,和Peyer’s貼劑。Fingolimod (hydrochloride)還增強鞘氨醇轉(zhuǎn)運蛋白Abcb1和白三烯C4轉(zhuǎn)運蛋白Abcc1的活性,并抑制胞漿磷脂酶A2的活性。
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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: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:-20°C
穩(wěn)定性:≥?4年
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Fingolimod (hydrochloride)參考文獻:
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).