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-18075
    LPA2 antagonist 1
    		Inhibitor 98.63%
    LPA2 antagonist 1 is a LPA2 antagonist with an IC50 of 17 nM.
    LPA2 antagonist 1
  • HY-107615
    TC LPA5 4
    		Antagonist 99.69%
    TC LPA5 4 is a LPA5 (GPR92)-specific non-lipid antagonist. TC LPA5 4 inhibits LPA-induced aggregation of isolated human platelet (LPA5-RH7777 cell line) with an IC50 of 800 nM. TC LPA5 4 displays selectivity for LPA5 over 80 other screened agent targets. TC LPA5 4 inhibits cell proliferation and migration of thyroid cancer cells.
    TC LPA5 4
  • HY-107616
    H2L5186303
    		Antagonist 98.72%
    H2L5186303 is an effective and selective LPA2 receptor antagonist, with an IC50 of 9 nM, and it has anti-inflammatory effects. H2L5186303 can inhibit intestinal cell proliferation and promote apoptosis.
    H2L5186303
  • HY-108495
    CYM50308
    		Agonist ≥98.0%
    CYM50308 (ML248) is a potent, selective and high affinity sphingosine-1-phosphate receptor 4 (S1P4-R) agonist with an EC50 of 56 nM. CYM50308 displays 37-fold more selective for S1P4-R than S1P5-R. CYM50308 has no activity at S1P1-R, S1P2-R and S1P3-R subtypes at concentrations up to 25 μM.
    CYM50308
  • HY-108490
    VPC 23019
    		Modulator 99.90%
    VPC 23019, an aryl amide-containing Sphingosine 1-phosphate (S1P) analog, is a competitive antagonist at the S1P1 and S1P3 receptors (pKi= 7.86 and 5.93, respectively) and an agonist at the S1P4 and S1P5 receptors (pEC50= 6.58 and 7.07, respectively).
    VPC 23019
  • HY-114379
    AS2717638
    		Antagonist 99.53%
    AS2717638 is a highly selective, brain-penetrant and orally active lysophosphatidic acid receptor 5 (LPA5) antagonist with an IC50 value of 38 nM. AS2717638 is highly selective and shows no significant antagonistic activity against other LPA receptors (LPA1, LPA2, and LPA3). AS2717638 can be used in the research of pain and neuroinflammation-related diseases.
    AS2717638
  • HY-139310
    GLPG2938
    		Antagonist 99.93%
    GLPG2938 is a potent and selective S1P2 antagonist. GLPG2938 can be used for the research of idiopathic pulmonary fibrosis.
    GLPG2938
  • HY-16734A
    Amiselimod hydrochloride
    		Agonist 98.71%
    Amiselimod (MT-1303) hydrochloride is converted to its active metabolite Amiselimod phosphate by sphingosine kinases in vivo. Amiselimod hydrochloride 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 hydrochloride inhibits chronic colitis via inhibiting infiltration of colitogenic Th1 and Th17 cells into the colon. Amiselimod hydrochloride inhibits lupus nephritis by reducing the infiltration of autoreactive T cells into the kidneys. Amiselimod hydrochloride is promising for research of autoimmune diseases.
    Amiselimod hydrochloride
  • HY-100619A
    BMS-986020 sodium
    		Inhibitor 99.41%
    BMS-986020 (AM152) sodium is a high-affinity lysophosphatidic acid receptor 1 (LPA1) antagonist. BMS-986020 sodium 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 sodium has the potential for the treatment of idiopathic pulmonary fibrosis (IPF).
    BMS-986020 sodium
  • HY-19511
    GSK2018682
    		Agonist 99.39%
    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-12288A
    Ozanimod hydrochloride
    		Modulator 99.19%
    Ozanimod (RPC-1063) hydrochloride, a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity selectively to S1P receptor subtypes 1 (S1P1) and 5 (S1P5). Ozanimod hydrochloride has modulate effect for hS1P1 and hS1P5 receptor with EC50s of 1.03 nM and 8.6 nM, respectively. Ozanimod hydrochloride can be used for the research of relapsing multiple sclerosis (MS) .
    Ozanimod hydrochloride
  • HY-17606
    Cenerimod
    		Agonist 99.43%
    Cenerimod (ACT-334441) is a potent, selective and orally active S1P1 receptor modulator, with an EC50 of 1 nM. Cenerimod shows more than 36 fold selctivity for hS1P1 over hS1P2, hS1P3, hS1P4, and hS1P5 receptor subtypes (EC50s=>10000, 228, 2134, and 36 nM, respectively). Cenerimod can attenuate murine experimental autoimmune encephalomyelitis (EAE) and murine sclerodermatous.
    Cenerimod
  • HY-150204
    ONO-0740556
    		Agonist 99.67%
    ONO-0740556 is a potent Gi-coupled human lysophosphatidic acid receptor 1 (LPA1) agonist with an EC50 value of 0.26 nM.
    ONO-0740556
  • HY-108494
    CYM50260
    		Agonist 99.70%
    CYM50260 is a potent and exquisitely selective sphingosine-1-phosphate 4 receptor (S1P4-R) agonist with an EC50 of 45 nM. CYM50260 displays no activity against S1P1-R, S1P2-R, S1P3-R and S1P5-R.
    CYM50260
  • HY-126145
    S1PR1 modulator 1
    		Inhibitor 99.44%
    S1PR1 modulator 1 is a selective S1PR1 inhibitor, with a pIC50 of 7.6, with >40- and >80-fold selectivity, over the other S1PR isoforms S1PR2/3/4.
    S1PR1 modulator 1
  • HY-114380
    Radioprotectin-1
    		Agonist 99.30%
    Radioprotectin-1 is a potent and specific nonlipid agonist of lysophosphatidic acid receptor 2 (LPA2), with an EC50 value of 25 nM for murine LPA2 subtype.
    Radioprotectin-1
  • HY-13660
    Mocravimod hydrochloride
    		Agonist 99.68%
    Mocravimod hydrochloride (KRP-203), an immunosuppressant, is a potent and orally active S1PR1 (sphingosine 1-phosphate receptor type 1) agonist.
    Mocravimod hydrochloride
  • 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-150254A
    SLB1122168 formic
    		Inhibitor 99.91%
    SLB1122168 formic is a potent Spns2-mediated S1P release inhibitor with an IC50 of 94 nM.
    SLB1122168 formic
  • HY-100676
    GRI977143
    		Agonist 99.84%
    GRI977143 is a specific LPA2 receptor agonist, with an EC50 of 3.3 μM .
    GRI977143
Cat. No. Product Name / Synonyms Application Reactivity
LPL Receptor Isoform Comparison

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