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-108496S
    Sphingosine-1-phosphate-d7
    		Agonist ≥99.0%
    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-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-128127
    NAEPA
    		Agonist ≥99.0%
    NAEPA, a phosphate-mimetic derivative, is a lysophosphatidic acid (LPA) receptor agonist.
    NAEPA
  • HY-10569S
    Ponesimod-d4
    		Agonist
    Ponesimod-d4 (ACT-128800-d4)is the deuterium labeledPonesimod(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-111021A
    ASP-4058 hydrochloride
    		Agonist 99.71%
    ASP-4058 hydrochloride is a next-generation, selective and orally active agonist for Sphingosine 1-Phosphate receptors 1 and 5 (S1P1 and S1P5), ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile.
    ASP-4058 hydrochloride
  • HY-148198
    S1P5 receptor agonist-1
    		Agonist
    S1P5 receptor agonist-1 (example 6) is a potent and selective agonist of S1P5 receptor with an EC50 value of 20 nM.
    S1P5 receptor agonist-1
  • HY-15425B
    PF-543 hydrochloride
    		Inhibitor
    PF-543 hydrochloride (Sphingosine Kinase 1 Inhibitor II hydrochloride) 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 hydrochloride is >100-fold selectivity for SPHK1 over SPHK2. PF-543 hydrochloride is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 hydrochloride induces apoptosis, necrosis, and autophagy.
    PF-543 hydrochloride
  • HY-19989
    MK-571
    		Inhibitor
    MK-571 (L-660711) 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 is also a MRP4 and ABCC1 (MRP1) inhibitor. MK-571 inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release.
    MK-571
  • HY-109038
    Mocravimod
    		Modulator
    Mocravimod is an oral activity amphematoshenol-1-1-phosphate receptor (S1PR) regulator, which can block the required signal from lymph organs to prevent the migration of effect cells from migrating to non-lymph hematopoietic tissue. Mocravimod can be used for cancer research.
    Mocravimod
  • HY-132847
    Vibozilimod
    		Agonist 99.52%
    Vibozilimod (SCD-044, example 33) is a S1p1 receptor agonist (extracted from patent WO2012140020A1).
    Vibozilimod
  • 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-10968A
    CYM5442 hydrochloride
    		Agonist
    CYM5442 hydrochloride is a potent, highly-selective and orally active sphingosine 1-phosphate (S1P1) receptor agonist with an EC50 of 1.35 nM. CYM5442 hydrochloride is inactive against S1P2, S1P3, S1P4, and S1P5. CYM5442 hydrochloride activates S1P1-dependent p42/p44-MAPK phosphorylation. CYM5442 exerts retinal neuroprotection. CYM5442 hydrochloride can easily penetrate the central nervous system (CNS).
    CYM5442 hydrochloride
  • HY-125881
    ASP1126
    		Agonist
    ASP1126 is a selective and orally active sphingosine-1-phosphate (S1P) agonist, with EC50 values of 7.12 nM, 517 nM for hS1P1 and hS1P3, respectively. ASP1126 decreases the number of peripheral lymphocytes, naive T cells, central memory T cells and effector memory T cells in the peripheral blood. ASP1126 has the potential to be applied in clinical transplantation with improved safety profile.
    ASP1126
  • HY-12355A
    Siponimod hemifumarate
    		Agonist
    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-148115
    S1p receptor agonist 2
    		Agonist
    S1p receptor agonist 2 (compound 1) is an agonist of S1P5 receptor, exhibits selectivity over the S1P1 and/or S1P3 receptors. S1p receptor agonist 2 can be used for endogenous SIP signaling system research, and alleviating or preventing CNS disorders research, such as neurodegenerative disorders.
    S1p receptor agonist 2
  • HY-11063S1
    Fingolimod-d4 hydrochloride
    		Antagonist ≥99.0%
    Fingolimod-d4 (hydrochloride) is the deuterium labeled Fingolimod hydrochloride. Fingolimod hydrochloride (FTY720) is a sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod hydrochloride (FTY720) also is a pak1 activator, a immunosuppressant[1].
    Fingolimod-d<sub>4</sub> hydrochloride
  • HY-149004A
    SLF1081851 TFA
    		Inhibitor
    SLF1081851 (TFA) is a Spns2 inhibitor, inhibits S1P release (IC50=1.93 μM). SLF1081851 (TFA) plays a key role in development and immune system.
    SLF1081851 TFA
  • HY-145362
    S1P1 agonist 4
    		Modulator
    S1P1 agonist 4 has a better profile in both potency (EC50 < 0.05 mg/kg) and predicted human half-life (t1/2 ∼ 5 days).
    S1P1 agonist 4
  • HY-156408
    Spns2-IN-1
    		Inhibitor
    Spns2-IN-1 is a potent inhibitor of Spns2-dependent S1P transport (Spns2), with IC50 of 1.4±0.3 μM that plays an important role in immune response.
    Spns2-IN-1
  • 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>
Cat. No. Product Name / Synonyms Application Reactivity
LPL Receptor Isoform Comparison

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