s1p5-r

CYM50308 is a high affinity agonist of sphingosine-1-phosphate receptor 4 (S1P4-R) (EC50: 56 nM). CYM50308 has no activity at S1P1-R, S1P2-R and S1P3-R subtypes at concentrations up to 25 μM and it shows 37-fold more selective for S1P4-R than S1P5-R.

Cenerimod (ACT-334441) is an orally active, selective, and potent sphingosine 1-phosphate receptor (S1P1) agonist (EC50: 1 nM).Cenerimod inhibits multiple S1P isoforms and can be used to study murine experimental autoimmune encephalomyelitis (EAE) and murine scleroderma.

S1PR5-IN-1 (Compound 7a) is a selective S1PR5 inhibitor capable of crossing the blood-brain barrier, with an IC50 of 85.4 nM. It exhibits exceptional binding affinity to S1PR5, with Kd values of 2.2 nM for recombinant human S1PR5 cell membranes, 4.6 nM for C57BL/6 mouse brains, and 27.6 nM for human cerebral cortex. S1PR5-IN-1 is applicable in researching neurodegenerative diseases such as multiple sclerosis.

CYM-5478 is a potent and selective S1P2 agonist that significantly increases the viability of C6 cells in a dose-dependent manner at concentrations above 100 nM under nutrient-deprivation stress (produced by serum-starvation).

Ponesimod (ACT-128800) is an orally available sphingosine-1-phosphate receptor 1 (S1PR1, S1P1) agonist with potential immunomodulating activity.

Ozanimod hydrochloride (RPC-1063 hydrochloride) is an orally available, selective and potent sphingosine 1-phosphate (S1P) receptor modulator that shows high affinity for S1P1 and S1P5.Ozanimod has potential anticancer activity and can be used in the study of multiple sclerosis (MS), ulcerative multiple sclerosis (UMS), and other diseases. (MS), ulcerative colitis, coronavirus infections and myelodysplasia.

BAF312 (Siponimod (BAF-312)), a next-generation S1P receptor modulator, is specific for S1P1 and S1P5 receptors with EC50 of 0.39 nM and 0.98 nM, respectively. The specificity of BAF312 for S1P1 and S1P5 receptors exhibits >1000-fold over S1P2, S1P3 and S1P4 receptors.

Siponimod (BAF-312) hemifumarate, a selective and potent modulator of sphingosine-1-phosphate (S1P) receptors, can be used in the study of multiple sclerosis (MS).

Ozanimod (RPC-1063) (RPC1063) is a specific oral S1P Receptor 1 modulator. Ozanimod has been used in trials studying the treatment of Crohn's Disease, Ulcerative Colitis, Multiple Sclerosis, and Relapsing Multiple Sclerosis.

S1P5 Receptor Agonist-1 (example 6) is a highly potent and selective agonist for the S1P5 receptor, exhibiting an EC50 value of 20 nM.

RP101442, the active metabolite of Ozanimod, is a selective and potent agonist of the sphingosine-1-phosphate receptor 1 (S1PR1), displaying EC50 values of 2.6 nM for S1PR1 and 171 nM for S1PR5.

RP101988, the principal active metabolite of Ozanimod, is a potent and selective agonist for sphingosine-1-phosphate receptor 1 (S1PR1), exhibiting half-maximal effective concentrations (EC50s) of 0.19 nM for S1PR1 and 32.8 nM for S1PR5.

CYM50260 is a potent and highly selective agonist of the sphingosine-1-phosphate 4 receptor (S1P4-R, EC50= nM), exhibiting no activity against S1P1-R, S1P2-R, S1P3-R, and S1P5-R.