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

LPL Receptor

Lysophospholipid Receptor

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-128127
    NAEPA
    Agonist ≥99.0%
    NAEPA, a phosphate-mimetic derivative, is a lysophosphatidic acid (LPA) receptor agonist.
    NAEPA
  • HY-P99318
    Sonepcizumab
    Inhibitor
    Sonepcizumab (LT 1009) is a fully human anti-S1P monoclonal antibody. Sonepcizumab has the potential for the research of metastatic renal cell carcinoma (mRCC).
    Sonepcizumab
  • 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-101939A
    RP-001 hydrochloride
    Agonist 98.8%
    RP-001 hydrochloride is a picomolar short-acting S1P1 (EDG1) selective agonist, with an EC50 of 9 pM. RP-00 hydrochloride induces internalization and polyubiquitination of S1P1. RP-001 hydrochloride has little activity on S1P2-S1P4 and only moderate affinity for S1P5.
    RP-001 hydrochloride
  • 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-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
  • HY-111021
    ASP-4058
    Agonist 99.54%
    ASP-4058 is a next-generation, selective and oral bioactive agonist for Sphingosine 1-Phosphate receptors 1 and 5 (S1P1 and S1P5), ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile.
    ASP-4058
  • HY-164964
    TRV045
    Agonist 98.15%
    TRV045 is a selective Sphingosine-1-phosphate subtype 1 receptor agonist with no effect on lymphocyte transport. TRV045 has antiepileptic activity.
    TRV045
  • HY-117959
    TAK-615
    Inhibitor 98.97%
    TAK-615 is a negative allosteric modulator (NAM) of the LPA1 receptor for the research of pulmonary fibrosis. TAK-615 binds the LPA1 receptor with high affinity (Kd high affinity of 1.7 nM and Kd low affinity of 14.5 nM).
    TAK-615
  • 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-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
  • HY-138453
    ACT-1016-0707
    Antagonist 98.28%
    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-14370
    LX2931
    Inhibitor 98.31%
    LX2931 is an inhibitor of Sphingosine 1-Phosphate Lyase (S1PL). LX2931 works by increasing levels of S1P inside and outside the cell. The decrease in S1PL activity leads to a significant increase in S1P content in tissues, especially in lymphoid tissues which may lead to a restricted exodus of lymphocytes from secondary immune tissues, resulting in lymphocytopenic and immunosuppressive effects in the peripheral circulation. LX2931 can be used in research for the treatment of autoimmune diseases, especially rheumatoid arthritis.
    LX2931
  • 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-136576
    RP101075
    Agonist 99.19%
    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-12355A
    Siponimod hemifumarate
    Agonist 99.64%
    Siponimod (BAF-312) hemifumarate is a potent and selective sphingosine-1-phosphate (S1P) receptor modulator. Siponimod hemifumarate is selective for S1P1 and S1P5 receptors over S1P2, S1P3, and S1P4 (EC50s of 0.39, 0.98, >10000, >1000, and 750 nM, respectively). Siponimod hemifumarate can be used for multiple sclerosis (MS) research.
    Siponimod hemifumarate
  • HY-RS12391
    S1PR1 Human Pre-designed siRNA Set A
    Inhibitor

    S1PR1 Human Pre-designed siRNA Set A contains three designed siRNAs for S1PR1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    S1PR1 Human Pre-designed siRNA Set A
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