Fingolimod 是一种 1-磷酸鞘氨醇 (S1P) 拮抗剂,作用于 K562 和 NK 细胞,IC50为 0.033 nM。它还是PAK1激活剂和免疫抑制剂。
产品描述
Fingolimod is an antagonist of sphingosine 1-phosphate (S1P) (IC50 of 0.033 nM in K562 and NK cells).
体外活性
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[1]
细胞实验
Sciatic nerve crush was performed in wildtype C57BL/6, in immunodeficient Rag1 (-/-) and Foxn1 (-/-) mice.?Analyses were based on walking track analysis and electrophysiology, histology, and cAMP formation.?Quantification of different LPA species was performed by liquid chromatography coupled to tandem mass spectrometry.?Furthermore, functional consequences of autotaxin inhibition by the specific inhibitor PF-8380 and the impact of fingolimod on early cytokine release in the injured sciatic nerve were investigated[1].
Cas No.
162359-55-9
分子式
C19H33NO2
分子量
307.478
别名
芬戈莫德;2-氨基-2-[2-(4-辛基苯基)乙基]-1,3-丙二醇;FTY-720A;FTY-720
储存和溶解度
Ethanol:7.69 mg/mL (25.01 mM),Need ultrasonic
Methanol:30 mg/mL (97.57 mM),Need ultrasonic
DMSO:66.67 mg/mL (216.83 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years