S1PR2 Agonist

Siponimod (BAF-312) is an orally active, blood-brain barrier penetrant dual agonist of S1P1/S1P5, with EC₅₀ values of 0.39 nM and 0.98 nM, respectively. Siponimod induces S1P1 internalization, activates GIRK channels, inhibits lymphocyte egress, reduces peripheral lymphocyte counts, triggers transient bradycardia, prevents synaptic neurodegeneration, promotes remyelination, alleviates demyelination, and prevents the loss of GABAergic interneurons. Siponimod can be used in research related to multiple sclerosis.

CYM-5478 is a potent and highly selective S1P₂ agonist with an EC₅₀ of 119 nM in a TGFα-shedding assay. CYM-5478 protects neural-derived cell lines against Cisplatin toxicity.

Siponimod (BAF-312) hemifumarate is an orally active, blood-brain barrier penetrant dual agonist of S1P1/S1P5, with EC₅₀ values of 0.39 nM and 0.98 nM, respectively. Siponimod hemifumarate induces S1P1 internalization, activates GIRK channels, inhibits lymphocyte egress, reduces peripheral lymphocyte counts, triggers transient bradycardia, prevents synaptic neurodegeneration, promotes remyelination, alleviates demyelination, and prevents the loss of GABAergic interneurons. Siponimod hemifumarate can be used in research related to multiple sclerosis.

L-threo Lysosphingomyelin (d18:1) (L-threo-Sphingosylphosphorylcholine) is an endogenous bioactive sphingolipid. L-threo Lysosphingomyelin (d18:1) is a potent S1P receptor agonist with EC₅₀s of 19.3, 131.8, and 313.3 nM for hS1P₁, hS1P₃, and hS1P₂, respectively.

XAX-162 is a highly selective sphingosine 1-phosphate receptor 2 (S1PR2) agonist with a human EC₅₀ of 0.55 μM. XAX-162 does not activate other S1P receptors. XAX-162 exhibits noncompetitive inhibition of activity by S1PR2 antagonist JTE-013 (HY-100675).