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CAS No. : 162359-55-9

MCE 國際站：Fingolimod

產(chǎn)品活性：Fingolimod 是一種 1-磷酸鞘氨醇 (sphingosine 1-phosphate，S1P) 拮抗劑，作用于 K562 和 NK 細胞，IC₅₀ 為 0.033 nM。Fingolimod 還是一種 pak1 激活劑，免疫抑制劑。

研究領(lǐng)域：GPCR/G Protein  |  Cytoskeleton  |  Cell Cycle/DNA Damage

作用靶點：LPL Receptor  |  PAK

In Vitro: 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.

In Vivo: 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 ¹⁸F-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 ¹⁸F-GE180 (P<0.0001) after treatment with Fingolimod.

相關(guān)產(chǎn)品：FDA-Approved Drug Library Plus  |  Drug Repurposing Compound Library  |  FDA-Approved Drug Library Mini  |  Anti-Aging Compound Library  |  Kinase Inhibitor Library  |  GPCR/G Protein Compound Library  |  CNS-Penetrant Compound Library  |  Anti-COVID-19 Compound Library  |  FDA-Approved Drug Library  |  Anti-Cancer Compound Library  |  Cell Cycle/DNA Damage Compound Library  |  Drug Repurposing Compound Library Plus  |  Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  FDA Approved & Pharmacopeial Drug Library  |  Fingolimod hydrochloride  |  PF-3758309  |  Ki16425  |  FRAX486  |  BMS-986020  |  Ozanimod  |  PF-543 Citrate  |  5-Aminosalicylic Acid  |  IPA-3  |  PF429242 dihydrochloride  |  TY-52156  |  G-5555  |  AM966  |  Etrasimod  |  AM095  |  FRAX1036  |  FRAX597  |  NVS-PAK1-1  |  Amiselimod hydrochloride  |  Cenerimod  |  LPA2 antagonist 1  |  FTY720 (S)-Phosphate  |  KPT-9274  |  ONO-7300243  |  S1p receptor agonist 1  |  Ponesimod  |  GNE 2861  |  CYM-5541

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