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

LPL 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.

LPL Receptor Isoform Specific Products:

  • LPAR2

  • S1PR1

  • S1PR2

  • S1PR3

  • S1PR4

  • S1PR5

LPL Receptor Related Products (41):

Cat. No. Product Name Effect Purity
  • HY-12005
    Fingolimod hydrochloride Modulator 99.86%
    Fingolimod hydrochloride (FTY720) is a sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod hydrochloride also is a pak1 activator.
  • HY-15425A
    PF-543 Citrate Inhibitor 98.10%
    PF-543 Citrate (Sphingosine Kinase 1 Inhibitor II Citrate) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 Citrate is >100-fold selectivity for SPHK1 over SPHK2. PF-543 Citrate is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 Citrate induces apoptosis, necrosis, and autophagy.
  • HY-12288
    Ozanimod Agonist 99.28%
    Ozanimod (RPC-1063) is a potent and selective S1P1 and S1P5 receptor agonist with EC50s of 410 pM and 11 nM in [35S]-GTPγS binding, respectively.
  • HY-13285
    Ki16425 Antagonist 98.67%
    Ki16425 (Debio 0719) is a subtype-selective, competitive antagonist of the EDG-family receptors, LPA1 and LPA3 with Kis of 0.34 μM and 0.93 μM, respectively. Ki16425 (Debio 0719) reduces the LPA-induced activation of p42/p44 MAPK. Ki16425 also can inhibits LPA-induced dephosphorylation of Yes-associated protein (YAP)/TAZ in HEK293A cells.
  • HY-100619
    BMS-986020 Antagonist 99.53%
    BMS-986020 is a high-affinity and selective lysophosphatidic acid receptor 1 (LPA1) antagonist. BMS-986020 inhibits bile acid and phospholipid transporters with IC50s of 4.8 µM, 6.2 µM, and 7.5 µM for BSEP, MRP4, and MDR3, respectively. BMS-986020 has the potential for the treatment of idiopathic pulmonary fibrosis (IPF).
  • HY-108496
    Sphingosine-1-phosphate Agonist >98.0%
    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.
  • HY-15425
    PF-543 Inhibitor
    PF-543 (Sphingosine Kinase 1 Inhibitor II) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 is >100-fold selectivity for SPHK1 over SPHK2. PF-543 is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 induces apoptosis, necrosis, and autophagy.
  • HY-136578
    RP101988 Agonist
    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.
  • HY-11063
    Fingolimod Antagonist 99.81%
    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.
  • HY-19736
    TY-52156 Antagonist 99.96%
    TY-52156 is a potent and selective S1P3 receptor antagonist with a Ki value of 110 nM.
  • HY-12789
    Etrasimod Antagonist 99.57%
    Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an IC50 value of 1.88 nM in CHO cells.
  • HY-15277
    AM966 Antagonist 99.85%
    AM966 is a high affinity, selective, oral LPA1-antagonist, inhibits LPA-stimulated intracellular calcium release (IC50=17 nM).
  • HY-100675
    JTE-013 Antagonist 99.57%
    JTE-013 is a potent and specific S1P2 (Sphingosine-1-Phosphate 2; EDG-5) antagonist. JTE-013 inhibits the specific binding of radiolabeled S1P to human and rat S1P2 with IC50s of 17 nM and 22 nM, respectively.
  • HY-16039
    AM095 Antagonist 99.72%
    AM095 is a selective LPA1 receptor antagonist. The IC50 for AM095 antagonism of LPA-induced calcium flux of human or mouse LPA1-transfected CHO cells is 0.025 and 0.023 μM, respectively.
  • HY-15382
    FTY720 (S)-Phosphate Agonist >98.0%
    FTY720 (S)-Phosphate is an agonist of S1P receptor 1 (S1PR1), used in the research of acute inflammatory diseases such as acute lung injury.
  • HY-18075
    LPA2 antagonist 1 Inhibitor 99.12%
    LPA2 antagonist 1 is a LPA2 antagonist with an IC50 of 17 nM.
  • HY-10569
    Ponesimod Agonist 99.72%
    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.
  • HY-16734A
    Amiselimod hydrochloride Agonist 99.02%
    Amiselimod hydrochloride is a novel sphingosine 1-phosphate receptor-1 (S1P1) modulator, designed to reduce the bradycardia effects associated with fingolimod and other S1P receptor modulators.
  • HY-100882
    ONO-7300243 Antagonist 98.14%
    ONO-7300243 is a novel, potent lysophosphatidic acid receptor 1 (LPA1) antagonist with IC50 of 0.16 μM.
  • HY-17606
    Cenerimod Agonist 98.02%
    Cenerimod (ACT-334441) is a potent and orally available sphingosine 1-phosphate 1 receptor (S1P1) agonist extracted from patent WO 2016184939 A1 and WO 2011007324 A1, example 1, with an EC50 of 2.7 nM.
Isoform Specific Products

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