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-114379
    AS2717638
    		Antagonist 99.53%
    AS2717638 is an oral active and selective lysophosphatidic acid receptor 5 (LPA5) antagonist, with an IC50 of 38 nM for hLPA5. AS2717638 also significantly improves PGE2-, PGF2α-, and AMPA-induced allodynia.
    AS2717638
  • HY-120797
    CRT0273750
    		98.50%
    CRT0273750 is an autotaxin (ATX) inhibitor and modulates LPA levels in plasm (IC50 = 0.014 μM). CRT0273750 can be used in ATX/LPA-dependent models of cancer.
    CRT0273750
  • 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-16040
    AM095 free acid
    		Inhibitor 98.24%
    AM095 (free acid) is a potent LPA1 receptor antagonist with IC50 values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 respectively.
    AM095 free acid
  • HY-115831
    SAR247799
    		Agonist
    SAR247799 (S1P1 agonist 3) is an oral activity, selective G-protein-biased sphingosine-1 phosphate receptor-1 (S1P1 ) agonist, with EC50s rang from 12.6 to 493 nM in S1P1-overexpressing cells and HUVECs. SAR247799 can be used for the research of endothelial protection, including type-2 diabetes, metabolic syndrome.
    SAR247799
  • HY-15706
    H2L 5765834
    		Antagonist 98.36%
    H2L 5765834 is an antagonist of lysophosphatidic acid receptors LPA1, LPA3, and LPA5, with IC50s of 94, 752, and 463 nM respectively.
    H2L 5765834
  • HY-18075
    LPA2 antagonist 1
    		Inhibitor 99.56%
    LPA2 antagonist 1 is a LPA2 antagonist with an IC50 of 17 nM.
    LPA2 antagonist 1
  • 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-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-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-100619A
    BMS-986020 sodium
    		Inhibitor 98.92%
    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-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-18641
    Ki16198
    		Antagonist 98.04%
    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-111021
    ASP-4058
    		Agonist 99.43%
    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-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-113973
    LPA2 antagonist 2
    		Antagonist
    LPA2 antagonist 2 (H2L 5226501) is a selective LPA2 antagonist with an IC50 of 28.3 nM and a Ki of 21.1 nM. LPA2 antagonist 2 is >480-fold more selective than LPA3 (IC50 of 13.85 μM).
    LPA2 antagonist 2
  • HY-101265
    Icanbelimod
    		Agonist 99.95%
    Icanbelimod (S1p receptor agonist 1) is a potent and orally active S1P receptor agonist, exhibits an activity of inducing S1P1 internalization (EC50=9.83 nM). Icanbelimod has the potential for the study of arthritis and EAE (experimental autoimmune encephalitis). Icanbelimod is extracted from patent WO2015039587A1, Compound 2.
    Icanbelimod
  • HY-100882
    ONO-7300243
    		Antagonist 98.46%
    ONO-7300243 is a novel, potent lysophosphatidic acid receptor 1 (LPA1) antagonist with IC50 of 0.16 μM.
    ONO-7300243
  • 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
LPL Receptor Isoform Comparison

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