NVP-AUY954 is an orally-available, benzothiazole-based, monoselective agonist of the sphingosine-1-phosphate receptor 1 (S1P1) intended for the treatment of human autoimmune mediated inflammatory neuropathies. Along with EC50 potency of 1.2 nM, NVP-AUY954 has at least 280-fold selectivity for S1P1 compared to the receptor's four other subtypes. (1, 2)
NVP-AUY954 induces a potent and reversible reduction of circulating lymphocytes; in combination with Everolimus, NVP-AUY954 can prolong the survival of cardiac allografts in a rat transplantation model. NVP-AUY954 also has been shown to activate downstream kinase cascades, increasing Erk (Tyr204) and Akt (Ser473) phosphorylation at EC50s of 0.1 and 1.0 nM, respectively. (2)
NVP-AUY954 efficacy has been correlated with an accumulation of plasmacytoid dendritic cells (pDC), which may have therapeutic value in the treatment of multiple sclerosis. (3)
Technical information:
| Chemical Formula: | C25H20F3NO2S | |
| CAS #: | 820240-77-5 | |
| Molecular Weight: | 455.49 | |
| Purity: | > 99% | |
| Appearance: | White | |
| Chemical Name: | 3-[[2-[4-phenyl-3-(trifluoromethyl)phenyl]-1-benzothiophen-5-yl]methylamino]propanoic acid | |
| Solubility: | Up to 50 mM in DMSO | |
| Synonyms: | NVP-AUY954, AUY954, AUY-954 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Zhang et al., AUY954, a selective S1P1 modulator, prevents experimental autoimmune neuritis. J. Neuroimmunol. 2009, 216, 59-65. Pubmed ID: 19804913 |
| 2. | Pan et al., A Monoselective Sphingosine-1-Phosphate Receptor-1 Agonist Prevents Allograft Rejection in a Stringent Rat Heart Transplantation Model. Chem. Biol. 2006, 13, 1227-1234. Pubmed ID: 17114004 |
| 3. | Galicia-Rosas et al., A Sphingosine-1-Phosphate Receptor 1-Directed Agonist Reduces Central Nervous System Inflammation in a Plasmacytoid Dendritic Cell-Dependent Manner. J. Immunol. 2012, 189, 3700-3706. Pubmed ID: 22933630 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
