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-12005
    Fingolimod hydrochloride
    Modulator 99.95%
    Fingolimod hydrochloride (FTY720), an analog of sphingosine, is a potent sphingosine 1-phosphate (S1P) receptors modulator. Fingolimod hydrochloride is phosphorylated by sphingosine kinases, particularly by SK2, and then binds S1PR1, 3, 4, and 5. Fingolimod hydrochloride induces the internalization of S1P1, and consequently, inhibits S1P activity. Fingolimod hydrochloride also is a pak1 activator.
    Fingolimod hydrochloride
  • 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.
    Sphingosine-1-phosphate
  • HY-19989A
    MK-571 sodium
    Inhibitor 99.24%
    MK-571 (L-660711) sodium is an orally active, potent and selective competitive leukotriene D4 (LTD4) receptor antagonist, with Ki values of 0.22 and 2.1 nM in guinea pig and human lung membranes, respectively. MK-571 sodium is also a inhibitor of multidrug resistance-associated protein MRP4 (ABCC4) and ABCC1 (MRP1). MK-571 sodium inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release.
    MK-571 sodium
  • HY-11063
    Fingolimod
    Antagonist 99.56%
    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
  • HY-D1005
    Poloxamer 407 (F127)
    Inhibitor
    Poloxamer 407 (F127) is a nonionic surfactant that is 100% active and relatively non-toxic to cells at low concentrations, and frequently used with dye AM esters such as Indo-1 AM, Fura-2 AM, Calcein AM, Fluo-3 AM, Fluo-4 AM, Quest Fluo-8™ AM and Quest Rhod-4™ AM, etc. to improve their water solubility. Poloxamer 407 is also a lipoprotein lipase inhibitor.
    Poloxamer 407 (F127)
  • HY-157787
    Ginkgolic acid 2-phosphate
    Agonist
    Ginkgolic acid 2-phosphate is a potent sphingosine 1-phosphate agonist. Ginkgolic acid 2-phosphate induces ERK phosphorylation. Ginkgolic acid 2-phosphate interactes with S1P1.
    Ginkgolic acid 2-phosphate
  • HY-12355S
    Siponimod-d11
    Modulator
    Siponimod-d11 is deuterium labeled Siponimod (HY-12355). Siponimod is an orally active and selective sphingosine-1-phosphate (S1P) receptor modulator. Siponimod is selective for S1P1 and S1P5 over S1P2, S1P3, and S1P4, with EC50s of 0.4, 0.98, >10000, >1000, and 750 nM, respectively. Siponimod can be used for multiple sclerosis (MS) research.
    Siponimod-d<sub>11</sub>
  • HY-W701470
    W140 hydrobromide
    Antagonist
    W140 hydrobromide is a S1P1 antagonist with the Ki of 2.84 μM, and can enhanceof capillary leakage and restoration of lymphocyte egress.
    W140 hydrobromide
  • HY-12355
    Siponimod
    Agonist 98.88%
    Siponimod (BAF-312) is an orally active and selective sphingosine-1-phosphate (S1P) receptor modulator. Siponimod is selective for S1P1 and S1P5 over S1P2, S1P3, and S1P4, with EC50s of 0.4, 0.98, >10000, >1000, and 750 nM, respectively. Siponimod can be used for multiple sclerosis (MS) research-.
    Siponimod
  • 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.
    JTE-013
  • HY-13285
    Ki16425
    Antagonist 98.11%
    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 can also inhibit LPA-induced dephosphorylation of Yes-associated protein (YAP)/TAZ in HEK293A cells.
    Ki16425
  • HY-12288
    Ozanimod
    Agonist 99.88%
    Ozanimod (RPC-1063), a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity selectively to S1P receptor subtypes 1 (S1P1) and 5 (S1P5). Ozanimod has modulate effect for hS1P1 and hS1P5 receptor with EC50s of 1.03 nM and 8.6 nM, respectively. Ozanimod can be used for the research of relapsing multiple sclerosis (MS).
    Ozanimod
  • HY-107614
    1-Oleoyl lysophosphatidic acid sodium
    Activator ≥98.0%
    1-Oleoyl lysophosphatidic acid (1-Oleoyl-sn-glycero-3-phosphate) sodium, a potent bioactive phospholipid, is a LPA receptor activator. 1-Oleoyl lysophosphatidic acid sodium can promote mitosis by inducing DNA synthesis. 1-Oleoyl lysophosphatidic acid sodium is also involved in normal and pathological emotional responses, including anxiety and depression.
    1-Oleoyl lysophosphatidic acid sodium
  • HY-15425A
    PF-543 Citrate
    Inhibitor 99.33%
    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.
    PF-543 Citrate
  • HY-100619
    BMS-986020
    Antagonist 99.91%
    BMS-986020 (AM152) 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).
    BMS-986020
  • HY-139853
    BMS-986278
    Antagonist 99.78%
    BMS-986278 is a potent and orally active lysophosphatidic acid receptor 1 (LPA1) antagonist, with Kbs of 6.9 nM and 4.0 nM for human and mouse LPA1, respectively. BMS-986278 can be used for the research of pulmonary fibrotic diseases.
    BMS-986278
  • HY-149004
    SLF1081851
    Inhibitor 98.11%
    SLF1081851 is a Spns2 inhibitor, inhibits S1P release (IC50=1.93 μM). SLF1081851 plays a key role in development and immune system.
    SLF1081851
  • HY-137862
    1-Oleoyl lysophosphatidic acid
    Activator ≥99.0%
    1-Oleoyl lysophosphatidic acid (1-Oleoyl-sn-glycero-3-phosphate) is an abundant lysophosphatidic acid (LPA) species with high biological activity due to its strong affinity for the LPA receptors. 1-Oleoyl lysophosphatidic acid is commonly used in most laboratories as a reagent for LPA receptor activation. 1-Oleoyl lysophosphatidic acid increases SRE-driven β-galactosidase activity.
    1-Oleoyl lysophosphatidic acid
  • HY-10569
    Ponesimod
    Agonist 99.81%
    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
  • HY-12789
    Etrasimod
    Antagonist 99.82%
    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.
    Etrasimod

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