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S1P Receptor

The sphingosine-1-phosphate receptors are a class of G protein-coupled receptors that are targets of the lipid signalling molecule Sphingosine-1-phosphate (S1P). They are divided into five subtypes: S1PR1, S1PR2, S1PR3, S1PR4 and S1PR5. .

  • Phorbol 12-myristate 13-acetate
    TQ019816561-29-8
    Phorbol 12-myristate 13-acetate (PMA) belongs to the phorbol ester group of natural products and is an activator of PKC, SphK, and NF-κB. Phorbol 12-myristate 13-acetate induces THP1 cell differentiation.
    • $44
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  • Ozanimod hydrochloride
    T625521618636-37-5
    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.
    • $61
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  • LX-2931
    T27864948840-25-3In house
    LX-2931(LX-3305) is a sphingosine-1-phosphate cleavage enzyme (S1P) inhibitor for the treatment of rheumatoid arthritis.
    • $258
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  • Ex26
    T286431233332-37-0
    Ex26 (S1P1-IN-Ex26) is a selective and potent sphingosine 1-phosphate receptor 1 (S1P1) antagonist that disrupts SR-B1-S1PR1 interactions and inhibits S1P-S1PR1 signaling.Ex26 can be used in experimental autoimmune encephalomyelitis, arterial Ex26 is used in experimental autoimmune encephalomyelitis, atherosclerosis and gastric cancer.
    • $113
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  • SLP9101555
    T63047 In house
    SLP9101555 is a potent and selective sphingosine kinase 2 (SphK2) inhibitor with a Ki of 90 nM.SLP9101555 has a high affinity for SphK2, which is 200-fold higher than that of SphK1.SLP9101555 dramatically reduces extracellular S1P sphingosine 1-phosphate (S1P) levels.
    • $350
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  • W140 HBr
    T602041246817-25-3In house
    [(3S)-3-amino-4-(3-hexylanilino)-4-oxobutyl]phosphonic acid;hydrobromide is a S1P1 antagonist with Ki of 2.84 μM.
    • $117
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  • BMS-960
    T268661265321-86-5In house
    BMS-960 is an S1P agonist with potential anti-tumour activity for cancer research.
    • $749
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  • ML-031
    T22101852230-33-2
    ML-031 activated S1P2 with an EC50 value of 1 μM in an S1P reporter assay.
    • $57
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  • ASP-4058
    T10385952565-91-2In house
    ASP-4058 is a selective, safe, and orally active second-generation agonist of sphingosine phosphate receptors 1 and 5 (S1P1 and S1P5).ASP-4058 ameliorates experimental autoimmune encephalomyelitis in mice.
    • $119
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  • Ceranib-2
    T107611402830-75-4In house
    Ceranib-2 (3-[(E)-3-(4-hydroxyphenyl)prop-2-enoyl]-4-phenyl-1H-quinolin-2-one) is an inhibitor of ceramidase with an IC50 of 28 μM in SKOV3 cells. Ceranib-2 decreases levels of sphingosine and S1P, induces cell apoptosis and exhibits anticancer activity.
    • $47
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  • K145 hydrochloride
    TQ01381449240-68-9In house
    K145 hydrochloride is a selective sphk2 inhibitor with substrate competitiveness and oral activity, with IC50 of 4.3 µM and Ki of 6.4 µM. K145 hydrochloride can induce apoptosis and has strong antitumor activity.
    • $50
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    TargetMol | Citations Cited
  • Ponesimod
    T3258854107-55-4
    Ponesimod (ACT-128800) is an orally available sphingosine-1-phosphate receptor 1 (S1PR1, S1P1) agonist with potential immunomodulating activity.
    • $38
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  • CYM5442
    T20261094042-01-9
    CYM5442 is an S1P agonist, targeting to Sphingosine.
    • $39
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  • Siponimod
    T64031230487-00-9
    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.
    • $33
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  • PF-543
    T60851415562-82-1
    PF-543 (Sphingosine Kinase 1 Inhibitor II), a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 and Ki of 2.0 nM and 3.6 nM.
    • $50
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  • PF-543 hydrochloride
    T88401706522-79-3
    PF-543 hydrochloride (PF-543) inhibits SphK1 with a K(i) of 3.6 nM, is sphingosine-competitive and is more than 100-fold selective for SphK1 over the SphK2 isoform.
    • $33
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  • Fingolimod
    T7939162359-55-9
    Fingolimod (FTY-720A) is an antagonist of sphingosine 1-phosphate (S1P) (IC50 of 0.033 nM in K562 and NK cells).
    • $50
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  • Vibozilimod
    T388261403232-33-6
    Vibozilimod (SCD-044) is S1P receptor-1 (S1PR1) agonist .
    • $113
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  • CS 2100
    T22697913827-99-3
    CS 2100 (1-[[4-Ethyl-5-[5-(4-phenoxyphenyl)-1,2,4-oxadiazol-3-yl]-2-thienyl]methyl]-3-azetidinecarboxylic acid) is an S1P1 agonist.
    • $41
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  • SphK1&2-IN-1
    T99921415662-57-5
    SphK1&2-IN-1 is a sphingosine kinase inhibitor with anti-inflammatory, antitumor and hemostatic effects.
    • $63
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  • AMG-369
    T299711202073-26-4
    AMG-369 (AMG 247) is an S1P1 S1P5 dual agonist that delays the onset of experimental autoimmune encephalomyelitis in rats. encephalomyelitis in rats.
    • $413
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  • SEW​2871
    T2171256414-75-2
    SEW 2871 is an orally available, highly selective S1P1 agonist with an EC50 of 13.8 nM.It reduces the number of lymphocytes in the blood and is used in studies related to diabetes, Alzheimer's disease, liver fibrosis, and inflammation. It activates ERK, Akt and Rac signaling pathways and induces S1P1 internalization and recycling.
    • $48
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  • TY-52156
    T17183934369-14-9
    TY-52156 is an effective and selective S1P3 receptor antagonist (Ki: 110 nM).
    • $34
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  • GSK2018682
    T73601034688-30-6
    GSK2018682 is an agonist of sphingosine-1-phosphate receptor (s1p1) and (s1p5) agonist(pEC50s of 7.7 and 7.2,respectively).
    • $30
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  • CYM50308
    T150321345858-76-5
    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.
    • $56
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  • MHP
    T46581104874-94-3
    MHP (Methyl caprooyl tyrosinate) is an activator of sphingosine kinase (SPHK1), and significantly stimulates CAMP mRNA and protein production in KC.
    • $39
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  • K6PC-5
    T27710756875-51-1
    K6PC-5 is a ceramide derivative that acts as an activator of sphingosine kinase 1 (SPHK1), inducing a swift and temporary rise in intracellular calcium levels. With its potential applications in skin diseases associated with abnormal keratinocyte function, as well as in studies on neurodegeneration and virus infection, K6PC-5 presents a promising compound for research purposes.
    • $34
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  • SK1-IN-1
    T129271218816-71-7
    SK1-IN-1 is a potent inhibitor of sphingosine kinase 1 (SPHK1)(IC50 of 58 nM).
    • $364
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  • Amiselimod hydrochloride
    T10305942398-84-7
    Amiselimod hydrochloride (MT-1303 hydrochloride) is a sphingosine 1-phosphate receptor-1 (S1P1) modulator.
    • $32
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  • PF429242 dihydrochloride
    T124372248666-66-0
    PF429242 dihydrochloride is a reversible and competitive inhibitor of S1P (IC50 of 175 nM).
    • $36
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  • 4-Deoxypyridoxine hydrochloride
    T38294148-51-6
    4-Deoxypyridoxine (4-DPD) is a vitamin B6 antimetabolite with diverse biological activities. It inhibits transport of pyridoxine , pyridoxal, and pyridoxamine in and reduces growth of S. carlsbergensis cells. 4-DPD inhibits sphingosine-1-phosphate (S1P) lyase and reduces cyclic stretch-induced apoptosis in alveolar epithelial MLE-12 cells. 4-DPD (5 mg, i.p.) reduces lysyl oxidase activity by 26% and reduces collagen and elastin crosslinking, resulting in limb abnormalities in chick embryos. It decreases latency to first seizure in mice (ED50 = 1 mmol/kg) and increases the occurrence and duration of myoclonic responses in baboons with photosensitive epilepsy. 4-DPD reduces TNF-α and IL-6 production in mice infected with T. spiralis.
    • $29
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  • Cenerimod
    T149241262414-04-9
    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.
    • $35
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  • Sphingosine-1-phosphate
    T2150026993-30-6
    Sphingosine-1-phosphate (S1P) is an agonist for S1P1-5 receptors and a ligand for GPR3, GPR6, GPR12.Sphingosine-1-phosphate is an intracellular second messenger that mobilises Ca2+ as an extracellular ligand for G-protein coupled receptors. Sphingosine-1-phosphate is an important lipid mediator generated from sphingosine (HY-113498) or other membrane phospholipids.
    • $299
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  • CYM-5541
    T3961945128-26-7
    CYM-5541 (ML249) is a selective and allosteric S1P3 receptor agonist.
    • $32
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  • VPC 23019
    T17237449173-19-7
    VPC 23019 is a competitive antagonist at the S1P1 and S1P3 receptors (pKi= 7.86 and 5.93, respectively). It is also an agonist at the S1P4 and S1P5 receptors (pEC50= 6.58 and 7.07, respectively).
    • $664
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  • Ozanimod
    T69231306760-87-1
    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.
    • $41
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  • Etrasimod
    TQ02271206123-37-6
    Etrasimod (APD334) is a specific and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor (IC50: 1.88 nM in CHO cells).
    • $48
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  • SKI V
    T846124418-86-8
    SKI V is a potent and noncompetitive non-lipid sphingosine kinase (SPHK; SK) inhibitor (GST-hSK,IC50 : 2 μM), and is a PI3K inhibitor(hPI3k,IC50 : 6 μM), induces apoptosis and has antitumor activity
    • $96
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  • SKI II
    T6673312636-16-1
    SKI II (SphK-I2) is a highly selective and non-ATP-competitive S1P receptor inhibitor (IC50: 0.5 μM) while exhibiting no inhibitory action on other kinases including PKCα, PI3K, and ERK2.
    • $39
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  • SKI-178
    T90141259484-97-3
    SKI-178 is a sphingosine kinase 1 (SphK1) inhibitor with IC50 of 0.1-1.8 μM. It induces prolonged mitosis followed by apoptotic cell death through the intrinsic apoptotic cascade. The sustained activation of CDK1 during prolonged mitosis, mediated by SKI-178 leads to the simultaneous phosphorylation of the prosurvival Bcl-2 family members, Bcl-2 and Bcl-xl, as well as the phosphorylation and subsequent degradation of Mcl-1.
    • $41
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  • MP-A08
    T16128219832-49-2
    MP-A08 is a highly selective ATP competitive inhibitor of sphingosine kinase (SPHK1) that targets both SphK1 and SphK2 (Ki: 6.9 ± 0.8 μM and 27 ± 3 μM, respectively).
    • $39
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  • Fingolimod hydrochloride
    T2539162359-56-0
    Fingolimod hydrochloride (FTY720) , a novel immune modulator, is a sphingosine 1-phosphate (S1P) antagonist (IC50: 0.033 nM in K562 and NK cells).
    • $35
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  • S1p receptor agonist 1
    T40311514888-56-2
    S1p receptor agonist 1 (S1p-receptor-agonist-1) is an S1P receptor agonist.
    • $39
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  • Opaganib
    T6750915385-81-8
    Opaganib (ABC294640) is an orally active and specific sphingosine kinase-2 (SphK2) inhibitor (IC50: 60 μM).
    • $34
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  • GLPG2938
    T91992130996-00-6
    GLPG2938 (1-(2-Ethoxy-6-(trifluoromethyl)pyridin-4-yl)-3-((5-methyl-6-(1-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl)pyridazin-3-yl)methyl)urea) is a potent and selective antagonist of S1P2.
    • $76
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  • JTE-013
    T15629383150-41-2
    JTE-013 is an effective and specific antagonist of S1P2. JTE-013 suppresses the specific binding of radiolabeled S1P to human and rat S1P2 (IC50s: 17 nM and 22 nM, respectively).
    • $70
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  • Peretinoin
    TQ006481485-25-8
    Peretinoin (NIK333) is an oral acyclic retinoid with a vitamin A-like structure that targets retinoid nuclear receptors such as RXR and RAR.
    • $34
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  • PF-543 Citrate
    T124361415562-83-2
    PF-543 Citrate is an inhibitor of sphingosine-competitive SPHK1(IC50 of 2 nM ).
    • $44
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  • CYM-5520
    T227031449747-00-5
    CYM-5520 is a noncompetitive allosteric agonist of S1P2
    • $40
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