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LPL Receptor

The lysophospholipid receptor (LPL-R) group are members of the G protein-coupled receptor family of integral membrane proteins that are important for lipid signaling. In humans, there are eight LPL receptors, each encoded by a separate gene. These LPL receptor genes are also sometimes referred to as "Edg" (an acronym for endothelial differentiation gene).

  • 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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  • 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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  • CYM50260
    T150311355026-60-6In house
    CYM50260 is a potent and exquisitely selective agonist of sphingosine-1-phosphate 4 receptor (S1P4-R, EC50= nM) with no activity against S1P1-R, S1P2-R, S1P3-R and S1P5-R.
    • $48
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  • S1PR1 modulator 1
    T128212328109-05-1In house
    S1PR1 modulator 1 is a selective inhibitor of S1PR1 with a pIC50 of 7.6.
    • $59
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  • 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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    TargetMol | Citations Cited
  • CYM5442
    T20261094042-01-9
    CYM5442 is an S1P agonist, targeting to Sphingosine.
    • $39
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    TargetMol | Citations Cited
  • Tyloxapol
    T030725301-02-4
    Tyloxapol (Triton WR1339) is a non-ionic liquid polymer used as a surfactant.
    • $30
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    TargetMol | Citations Cited
  • 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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    TargetMol | Citations Cited
  • 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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    TargetMol | Citations Cited
  • Spns2-IN-1
    T81114
    Spns2-IN-1 is a potent Spns2 inhibitor, effectively impeding Spns2-dependent S1P transport with an IC50 value of 1.4±0.3 μM, crucial for modulating the immune response [1].
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  • Ki16198
    T6347355025-13-7
    Ki16198 is an orally available LPA receptor antagonist and is a methyl ester derivative of Ki16425. It inhibits LPA1- and LPA3-induced inositol phosphates with Ki values of 0.34 and 0.93 μM, respectively, and can be used in studies of pancreatic carcinogenesis and metastasis.
    • $48
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  • (S)-FTY720-phosphonate
    T780911142015-10-8
    FTY720 (S)-Phosphate, an S1P receptor 1 (S1PR1) agonist, is utilized in studying acute inflammatory diseases, including acute lung injury.
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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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  • 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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  • 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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  • S1P1 agonist 6 hemicalcium
    T798172941310-03-6
    Compound I (S1P1 agonist 6 hemicalcium) is an S1P1 agonist that diminishes autoimmune activity by inhibiting lymphocyte trafficking, and serves as an immunosuppressive agent in researching a range of autoimmune diseases [1].
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  • SLB1122168 formic
    T78160
    SLB1122168 is a potent inhibitor of Spns2-mediated sphingosine-1-phosphate (S1P) release, exhibiting an IC50 value of 94 nM [1].
    • $130
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  • BMS-986020
    T40161257213-50-5
    BMS-986020 (AM152) is a selective antagonist of LPA1.
    • $47
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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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  • S1P1 agonist 6
    T798162433782-42-2
    Compound I (S1P1 agonist 6) is an S1P1 agonist that mitigates autoimmune activity by inhibiting lymphocyte trafficking and has potential as an immunosuppressive agent in autoimmune disease research [1].
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  • AM966
    T42781228690-19-4
    AM966, a excellent affinity, specific, oral LPA1(IC50=17 nM) antagonist, suppresses LPA-stimulated intracellular calcium release.
    • $34
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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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  • AM095 free acid
    T102931228690-36-5
    AM095 (free acid) is a potent LPA1 receptor antagonist (IC50s: 0.98 and 0.73 μM for recombinant human or mouse LPA1).
    • $33
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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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  • NIBR-0213
    T281691233332-14-3
    NIBR-0213, a potent and selective S1P(1) antagonist, has efficacy in experimental autoimmune encephalomyelitis.
    • $39
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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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  • 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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  • 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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  • CYM50358
    T94641314212-39-9
    N-(4-(aminomethyl)-2,6-dimethylphenyl)-5 is a potent, selective antagonist of the sphingosine-1-phosphate receptor 4 (S1P4). CYM50358 inhibits S1P4 with an IC50 of 25 nM.
    • $51
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  • AM095
    T20001345614-59-6
    AM095 is a potent LPA1 receptor antagonist with IC50 values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 respectively.
    • $41
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  • Ki16425
    T6108355025-24-0
    Ki16425 (Debio 0719) is a competitive, potent and reversible antagonist to LPA1, LPA2 and LPA3 with Ki of 0.34 μM, 6.5 μM and 0.93 μM, respectively.
    • $35
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  • SLF1081851
    T611122763730-97-6
    SLF1081851 is a Spns2 inhibitor. SLF1081851 inhibits S1P release with IC50 of 1.93 μM.
    • $51
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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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  • Mocravimod hydrochloride
    T12086509088-69-1
    Mocravimod hydrochloride (KRP-203) is an effecitive and orally active agonist of sphingosine 1-phosphate receptor type 1(S1PR1).
    • $64
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  • Sonepcizumab
    T768281031360-18-5
    Sonepcizumab (LT 1009) is a fully humanized monoclonal antibody against S1P. Sonepcizumab has anti-cancer activity and can be used to study metastatic renal cell carcinoma (mRCC) to prevent eye scarring after glaucoma filtration surgery.
    • $289
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  • H2L 5765834
    T22834420841-84-5
    H2L 5765834 is a lysophosphatidic acid receptors antagonist
    • $56
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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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  • ONO-7300243
    T7393638132-34-0
    ONO-7300243 is an antagonist of lysophosphatidic acid receptor 1 (LPA1; IC50 : 0.16 µM).
    • $38
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  • Ibrolipim
    T7832133208-93-2
    Ibrolipim (NO-1886) attenuates high glucose-induced endothelial dysfunction in cultured human umbilical vein endothelial cells via PI3K Akt pathway.
    • $43
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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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  • CYM-5520
    T227031449747-00-5
    CYM-5520 is a noncompetitive allosteric agonist of S1P2
    • $40
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