fty 720

Fingolimod hydrochloride (FTY720) , a novel immune modulator, is a sphingosine 1-phosphate (S1P) antagonist (IC50: 0.033 nM in K562 and NK cells).

Fingolimod (FTY-720A) is an antagonist of sphingosine 1-phosphate (S1P) (IC50 of 0.033 nM in K562 and NK cells).

FTY720 (S)-Phosphate is the active stereoisomeric phosphate derivative of FTY720 that acts as a potent modulator of sphingosine-1-phosphate (S1P) receptors. FTY720 (S)-Phosphate binds to S1P receptor subtypes S1P1, S1P3, S1P4, and S1P5 with Ki values of 2.1, 5.9, 23, and 2.2 nM respectively, causing receptor internalization on lymphocytes， preventing S1P-mediated lymphocyte egress from lymphoid tissues. FTY720 (S)-Phosphate also enhances endothelial barrier integrity, stimulates transporters such as Abcb1 and Abcc1, and inhibits cytosolic phospholipase A2 activity, highlighting its multifunctional pharmacological properties, making it an compound of interest in the research of diseases including multiple sclerosis, autoimmune diseases and cancer.

FTY720-C2 is an FTY720 analog. It acts as an effective stimulator of the activity of the protein phosphatase 2A.

Azido-FTY720 (azido-Fingolimod) is an analogue of FTY720 featuring an azido group suitable for click chemistry reactions. FTY720 is an orally available S1P analogue and S1P1R modulator capable of crossing the blood-brain barrier (BBB), reducing neuroinflammation, and is indicated for multiple sclerosis (MS).

(R)-FTY720-OMe is a structural analogue of FTY720 which acts as a specific competitive inhibitor of sphingosine kinase 2 (SK2). Furthermore, (R)-FTY720-OMe does not inhibit sphingosine kinase 1 (SK1) activity.

FTY720 (S)-Phosphate, an S1P receptor 1 (S1PR1) agonist, is utilized in studying acute inflammatory diseases, including acute lung injury.

FTY720, an immune modulator, down-regulates sphingosine-1-phosphate (S1P) receptors, enhances the activity of sphingosine transporter Abcb1 and leukotriene C4 transporter Abcc1, and inhibits cytosolic phospholipase A2 activity. Its efficacy relies on in vivo phosphorylation by sphingosine kinases, resulting in FTY720-phosphate which also down-regulates S1P receptors. NBD-FTY720, a fluorescently-labeled analog of FTY720, retains the hydroxy methyl side chain targeted for phosphorylation, suggesting potential phosphorylation in vivo.

MP07-66 is a novel FTY720-analog devoid of immunosuppressive effects leads to the reactivation of PP2A, which in turn triggers apoptosis of CLL cells.

(R)-FTY-720 Vinylphosphonate is a sphingosine 1-phosphate type 1 (S1P1) receptor agonist and lacks anti-apoptotic activity.

(S)-FTY-720 Vinylphosphonate inhibits sphingosine kinase 1 and promotes its proteasomal degradation in human pulmonary artery smooth muscle, breast cancer cells, and androgen-independent prostate cancer cells.

VPC03090 is a Sphingosine-1-Phosphate Receptor Inhibitor. VPC03090 is an analog of FTY-720, acts as antagonist for S1PR1 and S1PR3. VPC03090-P, converted from VPC03090 through the phosphorylation by SK-2, causes a reduction in tumor growth in mice with mammary cancer, and its oral bioavailability is determined to be 30 hours.