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抑制剂/激活剂

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凋亡与自噬

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Fingolimod 芬戈莫德; FTY720 free base

Fingolimod (FTY720 free base) 是一种 1-磷酸鞘氨醇 (sphingosine 1-phosphate，S1P) 拮抗剂，作用于 K562 和 NK 细胞，IC50 为 0.033 nM。Fingolimod 还是一种 pak1 激活剂，免疫抑制剂。

货号：
TK0281
规格：

10mg

25mg

100mg
价格：
￥0.00

产品参数

CAS No.	162359-55-9
生物活性	Fingolimod (FTY720 free base) is a sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator, a immunosuppressant.
分子式	C19H33NO2
分子量	307.47
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	H2O : 100 mg/mL (312.25 mM; Need ultrasonic) DMSO : 50 mg/mL (156.12 mM; Need ultrasonic) Methanol : 50 mg/mL (156.12 mM; Need ultrasonic)
体内研究	Fingolimod treatment results in significantly increased nerve conduction at 14 days post-crush in wildtype C57BL/6 mice. However, Foxn1 mice, which are devoid of T- but not B-lymphocytes, show an improvement of nerve regeneration under fingolimod treatment. Although the mean increase in nerve conduction velocity in both fingolimod-treated and controlFoxn1 mice implies a potentially positive role of T-lymphocyte deficiency on nerve regeneration, only fingolimod-treated Foxn1 mice show a significant improvement compared to C57BL/6 controls and performed better in the functional analysis. Treatment of the animals with Fingolimod for 28 d results in a clear reduction in the binding of F-GE180 when compare with vehicle-treated animals and evaluated by ex vivo autoradiography. Quantification of the binding of the radiotracer revealed a significant reduction in the binding potential of F-GE180 (P<0.0001) after treatment with Fingolimod.
体外研究	The monocyte-derived immature dendritic cells (iDCs) are pretreated with various concentrations of S1P for various periods of time prior to their incubation with NK cells. Four hours incubation of autologous or allogeneic iDCs with 0.2-20 μM of S1P significantly protectes these cells from NK cell lysis. The IC50 values of S1P are calculated at 160 nM for autologous iDCs, and 34 nM for allogeneic iDCs. Next, the inhibitory effect of S1P is revered by various concentrations of Fingolimod or SEW2871, with an IC50 effect of 173 or 15 nM, respectively. Fingolimod has been reported to reduce LPA synthesis via inhibition of the lysophospholipase autotaxin. Fingolimod treatment correlates with a significant elevation of axonal cAMP, a crucial factor for axonal outgrowth. Additionally, Fingolimod significantly reduces LPA levels in the injured nerve. PF-8380 treatment correlates with improved myelin thickness.
文献	•Nat Commun. 2022 Jan 10;13(1):182. •Theranostics. 2021 Jan 1;11(1):117-131. •Cancer Lett. 2018 Aug 16;436:75-86. •Haematologica. 2020 Mar;105(3):674-686. •Breast Cancer Res. 2017 Aug 4;19(1):90. •Commun Biol. 2021 Mar 25;4(1):399. •Front Pharmacol. 2018 Oct 31;9:1237. •Front Endocrinol (Lausanne). 2018 Mar 22;9:120. •Life Sci. 2019 Jan 15;217:243-250. •J Mol Cell Cardiol. 2021 Nov 10;S0022-2828(21)00210-8. •Int Immunopharmacol. 2021 Apr 26;96:107511. •Helicobacter. 2019 Oct;24(5):e12652. •PLoS Negl Trop Dis. 2019 Aug 20;13(8):e0007681. •J Gastroenterol Hepatol. 2018 Jan 15. •Vet Microbiol. 2021, 109177. •Patent. US20210393524A1.
纯度及产品资料	98%

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