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-N2553
    4-Deoxypyridoxine 5'-phosphate
    Inhibitor ≥98.0%
    4-Deoxypyridoxine 5'-phosphate is a Pyridoxal 5'-phosphate analogue and a sphingosine 1-phosphate (S1P) inhibitor. 4-Deoxypyridoxine 5'-phosphate inhibits ornithine decarboxylase activity with a Ki of 60 μM. 4-Deoxypyridoxine 5'-phosphate is a competitive inhibitor of the activation of glutamate apodecarboxylase by Pyridoxal 5'-phosphate (Ki of 0.27 μM) and strongly inhibits glutamate-dependent labeling of glutamate decarboxylase.
    4-Deoxypyridoxine 5'-phosphate
  • HY-117444
    ONO-9780307
    Inhibitor 99.94%
    ONO-9780307 is a specific synthetic LPA1 (lysophosphatidic acid receptor 1) antagonist with an IC50 value of 2.7 nM.
    ONO-9780307
  • HY-100882
    ONO-7300243
    Antagonist 98.46%
    ONO-7300243 is a novel, potent lysophosphatidic acid receptor 1 (LPA1) antagonist with IC50 of 0.16 μM.
    ONO-7300243
  • HY-136578
    RP101988
    Agonist 98.80%
    RP101988, the major active metabolite of Ozanimod, is a selective, potent S1PR1 (sphingosine-1-phosphate receptor 1) agonist, with EC50s of 0.19 nM and 32.8 nM for S1PR1 and S1PR5, respectivlely.
    RP101988
  • HY-132187
    Sphingosylphosphorylcholine
    99.50%
    Sphingosylphosphorylcholine is a bioactive sphingolipid. Sphingosylphosphorylcholine has anti-tumor activity.
    Sphingosylphosphorylcholine
  • 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.
    CYM-5478
  • HY-162655
    SLF80821178
    Inhibitor 99.70%
    SLF80821178 is a potent and orally active inhibitor of Sphingosine-1-Phosphate Transporter (Spns2). SLF80821178 inhibits S1P release with an IC50 of 51 nM in HeLa cells and a T1/2 of 2.4 h in mouse.
    SLF80821178
  • 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-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-18166
    NIBR0213
    Antagonist 99.38%
    NIBR-0213 is a potent, orally active and selective S1P1 antagonist with efficacy in experimental autoimmune encephalomyelitis. NIBR-0213 displays potent and comparable potency on human and rat S1P1 (IC50 of 2.0 nM and 2.3 nM, respectively) in GTPγ35S assays.
    NIBR0213
  • 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.
    CYM50179
  • HY-110291
    A-971432
    Agonist ≥99.0%
    A-971432 is a potent, selective and orally active sphingosine-1-phosphate (S1P) receptor 5 agonist with IC50s of .362, >10, 0.006 μM for S1P1, S1P3, S1P5 respectively. A-971432 protects blood–brain barrier (BBB) homeostasis. A-971432 reverses age-related cognitive decline. A-971432 has the potential for the research of alzheimer’s disease or multiple sclerosis .
    A-971432
  • HY-101265
    Icanbelimod
    Agonist 99.95%
    Icanbelimod (S1p receptor agonist 1) is a potent and orally active S1P receptor agonist, exhibits an activity of inducing S1P1 internalization (EC50=9.83 nM). Icanbelimod has the potential for the study of arthritis and EAE (experimental autoimmune encephalitis). Icanbelimod is extracted from patent WO2015039587A1, Compound 2.
    Icanbelimod
  • HY-139094
    A6770
    Inhibitor ≥99.0%
    A6770 is an orally active, potent sphingosine 1-phosphate (S1P) lyase (S1PL) inhibitor. A6770 is phosphorylated and the phosphorylated form directly inhibits S1P lyased.A6770, a potential key metabolite of THI, induces a [3H]dhS1P increase.
    A6770
  • 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-12685
    Ceralifimod
    Agonist 99.49%
    Ceralifimod (ONO-4641) is selective, high potent agonist for sphingosine 1-phosphate receptors 1 and 5, with EC50s of 27.3, 334 pM for human S1P receptor 1 and 5, respectively.
    Ceralifimod
  • HY-120478
    ASP6432
    Antagonist
    ASP6432 is a potent and selective type 1 lysophosphatidic acid receptor (LPA1) antagonist with IC50s of 11 nM and 30 nM for human LPA1 and rat LPA1, respectively.
    ASP6432
  • HY-147660
    IMMH001
    Agonist 98.10%
    IMMH001, also called SYL930, is an orally active, potent and selective S1P1 (sphingosine-1-phosphate receptor 1) agonist. IMMH001 decreased levels of both chemokines and proinflammatory cytokines, including IL-1β, IL-5, IL-18, IP10, CCL3, and CCL5. IMMH001 can be used for rheumatoid arthritis (RA) research.
    IMMH001
  • 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[1]. Sphingosine-1-phosphate is an important lipid mediator generated from Sphingomyelin (HY-113498) or other membrane phospholipids[2].
    Sphingosine-1-phosphate-d<sub>7</sub>
  • 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
Cat. No. Product Name / Synonyms Application Reactivity

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