Fingolimod

SKU: orb1299367

Description

Fingolimod (FTY-720) is a potent sphingosine 1-phosphate (S1P) receptor antagonist with an IC50 of 0.033 nM. It is widely used in research to investigate S1P signaling in immunology and neurology, with applications in both in vitro cell-based assays and in vivo models of autoimmune and inflammatory diseases.

Research Area

Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 162359-55-9
• MW: 307.47
• Purity: 99.76% (May vary between batches)
• Formula: C₁₉H₃₃NO₂
• SMILES: CCCCCCCCc1ccc(CCC(N)(CO)CO)cc1
• Target: S1P Receptor|||PAK|||LPL Receptor
• Solubility: DMSO:1 mg/mL (3.25 mM);Ethanol:7.69 mg/mL (25.01 mM);Methanol:30 mg/mL (97.57 mM)

Bioactivity

• Target IC50:
  S1P1:0.033 nM
• In Vitro:
  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
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• Cell Research:
  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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

p21 activated kinases, S1P Receptor, S1P, S1PReceptor, FTY 720, FTY720, FTY-720, FTY-720A, Fingolimod, Inhibitor, LPLReceptor, LPL Receptor, LPL, inhibit, PAK, Lysophospholipid Receptor

Compound Identifiers

PubChem CID

107970

Anthony W. Frei, Ying Li, Kaiyuan Jiang, Peter Buchwald, Cherie L. Stabler Local delivery of fingolimod from three‐dimensional scaffolds impacts islet graft efficacy and microenvironment in a murine diabetic model J Tissue Eng Regen Med, 12, 2 (2017)

PubMed: 28486786

Applications

In vitro

Reactivity

Rat