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-159983
    GS-2278
    		Antagonist 98.70%
    GS-2278 is an LPAR1 (lysophosphatidic acid receptor 1) antagonist with potential for research in idiopathic pulmonary fibrosis (IPF).
    GS-2278
  • HY-150254A
    SLB1122168 formic
    		Inhibitor 99.91%
    SLB1122168 formic is a Spinster Homolog 2 (Spns2) inhibitor. SLB1122168 formic inhibits Spns2-mediated sphingosine-1-phosphate (S1P) release with an IC50 of 94 nM. SLB1122168 formic induces lymphopenia in circulating lymphocytes in mice and rats.
    SLB1122168 formic
  • 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-18641
    Ki16198
    		Antagonist 98.17%
    Ki16198 is a potent and orally active LPA receptor antagonist, the methyl ester of Ki16425 (HY-13285). Ki16198 inhibits LPA1 and LPA3-induced inositol phosphate production with?Ki?values of 0.34 μM and 0.93 μM, respectively. Ki16198 is effective for pancreatic cancer tumorigenesis and metastasis in vivo.
    Ki16198
  • HY-176533
    S1PR5-IN-1
    		Inhibitor 99.58%
    S1PR5-IN-1 (Compound 7a) is a highly selective S1PR5 antagonist and orally bioavailable inhibitor with a human S1PR5 IC50 of 85.4 nM and human S1PR5 Ka of 2.173 nM.S1PR5-IN-1 binds to S1PR5 and inhibits natural killer cell migration toward sphingosine-1-phosphate.S1PR5-IN-1 can be used for the research of multiple sclerosis.
    S1PR5-IN-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-NP203
    High density lipoprotein (human)
    		Activator 98.00%
    High density lipoprotein (human) (HDL (human)) is a human-derived high-density lipoprotein. High density lipoprotein can cross the blood-brain barrier, and partially acts on endothelial nitric oxide synthase (eNOS) by activating surface receptors such as SR-B1 and S1P3R, as well as intracellular signaling cascades involving Akt, PI3K and MAPK, thereby inducing the production of NO in endothelial cells. High density lipoprotein (human) can be used in research related to type 2 diabetes, Alzheimer's disease, cancer and atherosclerosis.
    High density lipoprotein (human)
  • 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-18076
    LPA1 receptor antagonist 1
    		Antagonist 99.13%
    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-158783
    SACLAC
    		Inhibitor 99.70%
    SACLAC, a Ceramide analog, is a potent and covalent acid ceramidase (ASAH1; AC) inhibitor with a Ki of 97.1 nM. SACLAC effectively blocks AC activity and induces a decrease in sphingosine 1-phosphate (S1P) and total ceramide levels. SACLAC reduces the levels of splicing factor SF3B1 and alternative Mcl-1 mRNA splicing, increases pro-apoptotic Mcl-1S levels to induce apoptosis in acute myeloid leukemia (AML) cells. SACLAC reduces the leukemic burden in human AML xenograft mouse models.
    SACLAC
  • HY-128127
    NAEPA
    		Agonist ≥99.0%
    NAEPA, a phosphate-mimetic derivative, is a lysophosphatidic acid (LPA) receptor agonist.
    NAEPA
  • HY-145561
    Cudetaxestat
    		Inhibitor 98.32%
    Cudetaxestat (BLD-0409; PAT-409) is an orally active and noncompetitive autotaxin (ATX) inhibitor. Cudetaxestat inhibits the activity of ATX, reduces the production of LPA, and thereby blocks the signal transduction of the ATX-LPA axis. Cudetaxestat can still maintain nanomolar-level biochemical efficacy even when the concentration of the LPC substrate increases. Cudetaxestat can be used for the study of various diseases related to LPA including fibrosis, tumor metastasis, inflammation and autoimmune diseases, etc.
    Cudetaxestat
  • HY-19511
    GSK2018682
    		Agonist 98.02%
    GSK2018682 is an agonist for S1P1 and S1P5 receptor with pEC50s of 7.7 and 7.2, respectively, and has no agonist activity towards human S1P2, S1P3, or S1P4. GSK2018682 is used in the research of multiple sclerosis.
    GSK2018682
  • 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-N1423B
    Glycocholic acid hydrate
    		Activator
    Glycocholic acid hydrate is a bile acid derivative. Glycocholic acid hydrate downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid hydrate inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid hydrate modulates related bile acid receptor signaling. Glycocholic acid hydrate suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid hydrate can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).
    Glycocholic acid hydrate
  • HY-158417
    KSI-6666
    		Antagonist
    KSI-6666 is an orally active, competitive antagonist for sphingosine 1-phosphate receptor 1 (S1PR1), with an IC50 of 6.4 nM. KSI-6666 exhibits anti-inflammatory efficacy in autoimmune encephalomyelitis model and T cell transfer colitis model.
    KSI-6666
  • HY-117213
    Ex26
    		Antagonist 99.4%
    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-RS12394
    S1PR2 Human Pre-designed siRNA Set A
    		Inhibitor

    S1PR2 Human Pre-designed siRNA Set A contains three designed siRNAs for S1PR2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    S1PR2 Human Pre-designed siRNA Set A
  • HY-12355A
    Siponimod hemifumarate
    		Agonist 99.64%
    Siponimod (BAF-312) hemifumarate is an orally active, blood-brain barrier penetrant dual agonist of S1P1/S1P5, with EC50 values of 0.39 nM and 0.98 nM, respectively. Siponimod hemifumarate induces S1P1 internalization, activates GIRK channels, inhibits lymphocyte egress, reduces peripheral lymphocyte counts, triggers transient bradycardia, prevents synaptic neurodegeneration, promotes remyelination, alleviates demyelination, and prevents the loss of GABAergic interneurons. Siponimod hemifumarate can be used in research related to multiple sclerosis.
    Siponimod hemifumarate
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
LPL Receptor Isoform Comparison

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