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-18076
    LPA1 receptor antagonist 1
    		Antagonist 98.8%
    LPA1 receptor antagonist 1 is a highly selective Lysophosphatidic Acid receptor-1 (LPA1) antagonist with an IC50 of 25 nM.
    LPA1 receptor antagonist 1
  • 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-117213
    Ex26
    		Antagonist 99.0%
    Ex26 (S1P1-IN-Ex26) is a potent and selective sphingosine 1-phosphate receptor 1 (S1P1) antagonist (IC50=0.93 nM). Ex26 shows >3,000-fold selectivity for S1P1 over other Sphingosine 1-phosphate receptors. Ex26 can be used in experimental autoimmune encephalomyelitis reseach.
    Ex26
  • HY-162267
    LPAR1 antagonist 1
    		Antagonist
    LPAR1 antagonist 1 (compound 18) is a potent, oral active and selective LPAR1 antagonist with the IC50 of 3.3 nM. LPAR1 antagonist 1 can be used for study of fibrosis.
    LPAR1 antagonist 1
  • 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-RS12403
    S1PR5 Human Pre-designed siRNA Set A
    		Inhibitor

    S1PR5 Human Pre-designed siRNA Set A contains three designed siRNAs for S1PR5 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    S1PR5 Human Pre-designed siRNA Set A
    S1PR5 Human Pre-designed siRNA Set A
  • HY-132187S1
    Sphingosylphosphorylcholine-d7
    		99.90%
    Sphingosylphosphorylcholine-d7 is the deuterium labeled Sphingosylphosphorylcholine (HY-132187).
    Sphingosylphosphorylcholine-d<sub>7</sub>
  • HY-16734
    Amiselimod
    		Modulator
    Amiselimod (MT-1303) is converted to its active metabolite Amiselimod phosphate by sphingosine kinases in vivo. Amiselimod is an orally active and high selectivity sphingosine 1-phosphate receptor-1 (S1P1) agonist, designed to reduce the bradycardia effects associated with fingolimod and other S1P receptor modulators. Amiselimod inhibits chronic colitis via inhibiting infiltration of colitogenic Th1 and Th17 cells into the colon. Amiselimod inhibits lupus nephritis by reducing the infiltration of autoreactive T cells into the kidneys. Amiselimodis promising for research of autoimmune diseases.
    Amiselimod
  • HY-11063S
    Fingolimod-d4
    		Antagonist 99.11%
    Fingolimod-d4 is the deuterium labeled Fingolimod. 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-d<sub>4</sub>
  • HY-148801
    Tamuzimod
    		Modulator
    Tamuzimod is a potent immunomodulator. Tamuzimod has S1P Receptor modulatory activity with an EC50 of <1 μM.
    Tamuzimod
  • 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-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-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 an orally active and selective S1PR1/EDG1 agonist with an EC50 of less than 1 nM. Vibozilimod has immunomodulatory activity and can reduce the number of lymphocytes. Vibozilimod can be used in the research of inflammatory diseases such as psoriasis and atopic dermatitis.
    Vibozilimod
  • 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-135432
    Etrasimod arginine
    		Modulator
    Etrasimod arginine is an orally available S1P receptor modulator that is a potent full agonist of the S1P1 receptor and has partial agonist activity at S1P4. Etrasimod arginine reduces inflammation in a CD4+CD45RBhigh T cell-transferred mouse colitis model.
    Etrasimod arginine
  • 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-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
Cat. No. Product Name / Synonyms Application Reactivity
LPL Receptor Isoform Comparison

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