MW 343.9 Da, Purity >98%. Potent agonist at four sphingosine-1-phosphate (S1P) receptors (S1P1, S1P3, S1P4, and S1P5). Novel immunomodulator able to block T-cell egress from lymph nodes. Structural analog of sphingosine. Orally active in vivo.
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- Journal of medicinal chemistry 59:1003-202016Discovery of Tetrahydropyrazolopyridine as Sphingosine 1-Phosphate Receptor 3 (S1P3)-Sparing S1P1 Agonists Active at Low Oral Doses.Applications:Unspecified applicationReactive species:Unspecified reactive speciesEmmanuel H Demont et. al.PubMed 26751273
- Arthritis research & therapy 18:82016The CII-specific autoimmune T-cell response develops in the presence of FTY720 but is regulated by enhanced Treg cells that inhibit the development of autoimmune arthritis.Applications:Unspecified applicationReactive species:Unspecified reactive speciesDavid C Miller,Karen B Whittington,David D Brand,Karen A Hasty,Edward F RosloniecPubMed 26757712
- Nature reviews. Drug discovery 9:883-972010Fingolimod (FTY720): discovery and development of an oral drug to treat multiple sclerosis.Applications:Unspecified applicationReactive species:Unspecified reactive speciesVolker Brinkmann et. al.PubMed 21031003
- Transplantation 72:764-92001FTY720: altered lymphocyte traffic results in allograft protection.Applications:Unspecified applicationReactive species:Unspecified reactive speciesV Brinkmann,D D Pinschewer,L Feng,S ChenPubMed 11571432
Key facts
- CAS number
- 162359-56-0
- Purity
- > 98%
- Form
- Solid
- Molecular weight
- 343.9 Da
- Molecular formula
- C19H34ClNO2
- PubChem identifier
- 107969
- Nature
- Synthetic
Alternative names
CD363, CHEDG 1, D1S3362, ECGF 1, EDG 1, Endothelial differentiation G-protein coupled receptor 1, Endothelial differentiation sphingolipid G protein coupled receptor 1, FLJ58121, G protein coupled sphingolipid receptor, S1P receptor 1, S1P receptor Edg-1, S1P(1) receptor, S1P1, S1PR1_HUMAN, Sphingosine 1-phosphate receptor 1, Sphingosine 1-phosphate receptor Edg-1, Sphingosine 1phosphate receptor type 1 S1P1, g protein-coupled receptor edg-1, sphingolipid g-protein-coupled receptor 1
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MW 343.9 Da, Purity >98%. Potent agonist at four sphingosine-1-phosphate (S1P) receptors (S1P1, S1P3, S1P4, and S1P5). Novel immunomodulator able to block T-cell egress from lymph nodes. Structural analog of sphingosine. Orally active in vivo.
Key facts
- CAS number
- 162359-56-0
- Purity
- > 98%
- Form
- Solid
- Molecular weight
- 343.9 Da
- Molecular formula
- C19H34ClNO2
- PubChem identifier
- 107969
- Nature
- Synthetic
- Solubility
Soluble in DMSO to 100 mM.
Soluble in ethanol to 100 mM (with warming).
- Biochemical name
- Fingolimod hydrochloride
- Biological description
Potent agonist at four sphingosine-1-phosphate (S1P) receptors (S1P1, S1P3, S1P4, and S1P5). Novel immunomodulator able to block T-cell egress from lymph nodes. Structural analog of sphingosine. Orally active in vivo.
- Canonical SMILES
- CCCCCCCCC1=CC=C(C=C1)CCC(CO)(CO)N.Cl
- InChI
- InChI=1S/C19H33NO2.ClH/c1-2-3-4-5-6-7-8-17-9-11-18(12-10-17)13-14-19(20,15-21)16-22;/h9-12,21-22H,2-8,13-16,20H2,1H3;1H
- InChIKey
- SWZTYAVBMYWFGS-UHFFFAOYSA-N
- IUPAC name
- 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol;hydrochloride
Storage
- Shipped at conditions
- Ambient - Can Ship with Ice
- Appropriate short-term storage conditions
- -20°C
- Appropriate long-term storage conditions
- -20°C
- Storage information
- Store under desiccating conditions
Supplementary info
- This supplementary information is collated from multiple sources and compiled automatically.
- Activity summary
The S1P1 receptor also known as EDG1 is a G-protein-coupled receptor that plays a significant role in the sphingosine-1-phosphate (S1P) signaling pathway. With a molecular mass of approximately 43 kDa S1P1 is expressed in various tissues such as vascular endothelial cells immune cells and cardiac cells. The protein mediates the effects of sphingosine-1-phosphate a bioactive lipid that participates in various physiological processes.
- Biological function summary
S1P1 is involved in the regulation of immune cell trafficking and vascular stability. As a part of a receptor complex it activates intracellular signaling cascades that influence cell migration and vascular maturation. By binding to S1P S1P1 controls the egress of lymphocytes from lymphoid tissues indicating its important role in immune surveillance and response.
- Pathways
S1P1 serves as an important component in the S1P signaling pathway and the phosphoinositide 3-kinase (PI3K) pathway. In the S1P pathway it regulates endothelial cell barrier function and vascular maturation. In the PI3K pathway S1P1 influences cell survival and migration which relates it to protein kinases like Akt and other signaling molecules that further modify cellular responses.
- Associated diseases and disorders
S1P1 is implicated in multiple sclerosis (MS) and cancer progression. In MS S1P1 modulation affects lymphocyte trafficking which is the mechanism behind the action of fingolimod (FTY720) a therapeutic agent for the disease. S1P1 also connects to VEGF and other angiogenic factors in cancer where it influences tumor angiogenesis and metastasis. Understanding these connections highlights the potential for targeting S1P1 in therapeutic strategies for these conditions.
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Chemical Structure - Fingolimod (FTY720), S1P receptor modulator (ab142065)
2D chemical structure image of ab142065, Fingolimod (FTY720), S1P receptor modulator
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