2. Signaling Pathways
  3. GPCR/G Protein
  4. LPL Receptor
  5. S1PR4 Isoform

S1PR4

S1PR4 is an S1P-responsive G-protein-coupled receptor that regulates cell shape and motility through Gαi and Gα12/13 coupling[1]. In immune cells, S1PR4 transduces S1P effects on T-cell proliferation and cytokine secretion without signaling migration, distinguishing it from migration-dominant S1P receptor functions[2]. Mechanistically, S1PR4 deficiency affects dendritic-cell function and Th17-cell differentiation in a murine model[3]. S1PR4 is also required for plasmacytoid dendritic-cell differentiation, because S1PR4-deficient mice show reduced plasmacytoid dendritic-cell abundance across organs[4]. In human plasmacytoid dendritic cells, S1PR4 signaling preserves ILT7 surface expression and limits TLR7/9-induced IFN-α production[5]. In disease models, S1PR4 promotes nonalcoholic steatohepatitis by activating the NLRP3 inflammasome in hepatic macrophages[6]. Compared with related isoforms, S1PR4 shows a functional profile centered on immune-cell activation, cytokine control, dendritic-cell biology, and inflammasome-linked macrophage responses rather than broad chemotactic signaling[2][3][5][6]. For experimental applications, potent and selective S1P4 receptor agonists provide pharmacological tools to decipher S1P4 biological function and assess therapeutic utility[7].

S1PR4 Related Products (9):

Cat. No. Product Name Effect Purity
  • HY-12355
    Siponimod
    		Agonist 99.95%
    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.
  • HY-10569
    Ponesimod
    		Agonist 99.78%
    Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation.
  • HY-136462
    CYM50358
    		Antagonist 98.33%
    CYM50358 is a potent and selective S1PR4 antagonist, with an IC50 of 25 nM. CYM50358 can be used for the research of influenza infection.
  • HY-111253
    CYM-5478
    		Agonist 99.90%
    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.
  • HY-17606
    Cenerimod
    		Agonist 99.43%
    Cenerimod (ACT-334441) is a potent, selective and orally active S1P1 receptor modulator, with an EC50 of 1 nM. Cenerimod shows more than 36 fold selctivity for hS1P1 over hS1P2, hS1P3, hS1P4, and hS1P5 receptor subtypes (EC50s=>10000, 228, 2134, and 36 nM, respectively). Cenerimod can attenuate murine experimental autoimmune encephalomyelitis (EAE) and murine sclerodermatous.
  • HY-W040167
    VPC 23153
    		Agonist
    VPC 23153 is a S1P4 receptor agonist and vasoconstrictor. VPC 23153 activates the S1P4 receptor, thereby triggering vasoconstriction. VPC 23153 induces pulmonary artery contraction. VPC 23153 can be used in studies related to pulmonary arterial hypertension.
  • HY-176533
    S1PR5-IN-1
    		Inhibitor 99.58%
    S1PR5-IN-1 (Compound 7a) is a highly selective S1PR5 antagonist and orally bioavailable inhibitor with a human S1PR5 IC50 of 85.4 nM and human S1PR5 Kd of 2.173 nM.S1PR5-IN-1 binds to S1PR5 and inhibits natural killer cell migration toward sphingosine-1-phosphate.S1PR5-IN-1 can be used for the research of multiple sclerosis.
  • HY-116146
    CYM50179
    		Agonist
    CYM50179 (compound 22n) is a potent and selective S1P4-R (Sphingosine-1-phosphate4 receptor) agonist with an EC50 of 46 nM.
  • HY-12355A
    Siponimod hemifumarate
    		Agonist 99.64%
    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.