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

LPL Receptor

Lysophospholipid Receptor

LPL Receptor

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LPL Receptor (Lysophospholipid Receptor) 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". LPL receptor ligands bind to and activate their cognate receptors located in the cell membrane. Depending on which ligand, receptor, and cell type is involved, the activated receptor can have a range of effects on the cell. These include primary effects of inhibition of adenylyl cyclase and release of calcium from the endoplasmic reticulum, as well as secondary effects of preventingapoptosis and increasing cell proliferation. Type: LPAR1, LPAR2, LPAR3, LPAR4, LPAR5, LPAR6, S1PR1, S1PR2, S1PR3, S1PR4, S1PR5.

LPL Receptor Isoform Specific Products:

LPL Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-12835
    S1P1 agonist III
    		Agonist 99.64%
    S1P1 Agonist III is a potent and orally active S1P1 agonist with EC50 of 18 nM; no activity on S1P3.
    S1P1 agonist III
  • HY-108496S
    Sphingosine-1-phosphate-d7
    		Agonist 99.00%
    Sphingosine-1-phosphate-d7 is the deuterium labeled Sphingosine-1-phosphate. Sphingosine-1-phosphate (S1P) is an agonist of S1P1-5 receptors and a ligand of GPR3, GPR6 and GPR12.?Sphingosine-1-phosphate is an intracellular second messenger and mobilizes Ca2+ as an extracellular ligand for G protein-coupled receptors. Sphingosine-1-phosphate is an important lipid mediator generated from Sphingomyelin (HY-113498) or other membrane phospholipids.
    Sphingosine-1-phosphate-d<sub>7</sub>
  • HY-115450
    ONO-0300302
    		Antagonist 99.43%
    ONO-0300302 is an orally active and potent LPA1 (lysophosphatidic acid receptor 1) antagonist, with an IC50 of 0.086 μM. ONO-0300302 is a slow tight binding inhibitor, and its binding affinity increases with time, with Kd of 0.34 nM (37 °C, 2 h). ONO-0300302 can be used for benign prostatic hyperplasia (BPH) research.
    ONO-0300302
  • HY-11063R
    Fingolimod (Standard)
    		Antagonist
    Fingolimod (Standard) is the analytical standard of Fingolimod. This product is intended for research and analytical applications. Fingolimod (FTY720 free base) is a sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator, a immunosuppressant.
    Fingolimod (Standard)
  • HY-138453
    ACT-1016-0707
    		Antagonist 98.15%
    ACT-1016-0707 (Compound 49) is an orally active and selective LPA1 receptor antagonist. ACT-1016-0707 can be used for the research of fibrotic diseases.
    ACT-1016-0707
  • HY-108493
    CS-2100
    		Agonist 99.12%
    CS-2100 (Compound 10b) is a potent, selective, orally active and S1P3-sparing S1P1 agonist with an EC50 of 4.0 nM for human S1P1. CS-2100 shows in vivo immunosuppressive efficacy in rats with an ID50 (infective dose) of 0.407 mg/kg for HvGR.
    CS-2100
  • HY-151392
    LPA5 antagonist 2
    		Antagonist 99.62%
    LPA5 antagonist 2 (compound 65) is a high aqueous solubility LPA5 (lysophosphatidic acid receptor 5) antagonist. LPA5 antagonist 2 significantly attenuates nociceptive hypersensitivity and it can be used for the research of inflammatory and neuropathic pains.
    LPA5 antagonist 2
  • HY-158783
    SACLAC
    		Inhibitor 99.70%
    SACLAC, a Ceramide analog, is a potent and covalent acid ceramidase (ASAH1; AC) inhibitor with a Ki of 97.1 nM. SACLAC effectively blocks AC activity and induces a decrease in sphingosine 1-phosphate (S1P) and total ceramide levels. SACLAC reduces the levels of splicing factor SF3B1 and alternative Mcl-1 mRNA splicing, increases pro-apoptotic Mcl-1S levels to induce apoptosis in acute myeloid leukemia (AML) cells. SACLAC reduces the leukemic burden in human AML xenograft mouse models.
    SACLAC
  • HY-RS12394
    S1PR2 Human Pre-designed siRNA Set A
    		Inhibitor

    S1PR2 Human Pre-designed siRNA Set A contains three designed siRNAs for S1PR2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    S1PR2 Human Pre-designed siRNA Set A
    S1PR2 Human Pre-designed siRNA Set A
  • HY-128127
    NAEPA
    		Agonist ≥99.0%
    NAEPA, a phosphate-mimetic derivative, is a lysophosphatidic acid (LPA) receptor agonist.
    NAEPA
  • HY-136576
    RP101075
    		Agonist
    RP101075, an active metabolite of Ozanimod, is a potent, orally active S1PR (sphingosine-1-phosphate receptor 1) agonist, with an EC50 of 0.27 nM. RP101075 displays >100-fold selectivity over S1PR5 (EC50=5.9 nM) and >10000-fold over S1PR 2, 3, and 4. RP101075 displays superior cardiovascular safety profile.
    RP101075
  • HY-150254
    SLB1122168
    		Inhibitor
    SLB1122168 is a potent Spns2-mediated S1P release inhibitor with an IC50 of 94 nM.
    SLB1122168
  • HY-104069
    S1P1 agonist 1
    		Agonist 98.75%
    S1P1 Agonist 1 is a S1P1 agonist with immunomodulatory activities.
    S1P1 agonist 1
  • HY-113934
    L-threo Lysosphingomyelin (d18:1)
    		Agonist ≥98.0%
    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.
    L-threo Lysosphingomyelin (d18:1)
  • HY-111292
    CYM-5482
    		Agonist 98.29%
    CYM-5482 is a potent and selective agonist Sphingosine 1-phosphate receptor 2 (S1PR2) with an IC50 and EC50 of 1.0 and 1.03 μM. CYM-5482 has the potential for the research of cancer diseases.
    CYM-5482
  • HY-10569S
    Ponesimod-d4
    		Agonist
    Ponesimod-d4 (ACT-128800-d4) is the deuterium labeled Ponesimod (HY-10569). 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.
    Ponesimod-d<sub>4</sub>
  • HY-15382A
    (S)-FTY720-phosphonate
    		Agonist 99.91%
    FTY720 (S)-Phosphate is an agonist of S1P receptor 1 (S1PR1), used in the research of acute inflammatory diseases such as acute lung injury.
    (S)-FTY720-phosphonate
  • HY-113973
    LPA2 antagonist 2
    		Antagonist
    LPA2 antagonist 2 (H2L 5226501) is a selective LPA2 antagonist with an IC50 of 28.3 nM and a Ki of 21.1 nM. LPA2 antagonist 2 is >480-fold more selective than LPA3 (IC50 of 13.85 μM).
    LPA2 antagonist 2
  • HY-150614
    Autotaxin-IN-6
    		Inhibitor
    Autotaxin-IN-6 (compound 23) is a potent autotaxin (ATX) inhibitor with an IC50 value of 30 nM. Autotaxin-IN-6 can reduce cell migration. Autotaxin-IN-6 can be used for researching anticancer.
    Autotaxin-IN-6
  • HY-158417
    KSI-6666
    		Antagonist
    KSI-6666 is an orally active, competitive antagonist for sphingosine 1-phosphate receptor 1 (S1PR1), with an IC50 of 6.4 nM. KSI-6666 exhibits anti-inflammatory efficacy in autoimmune encephalomyelitis model and T cell transfer colitis model.
    KSI-6666
Cat. No. Product Name / Synonyms Application Reactivity
LPL Receptor Isoform Comparison

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