1. GPCR/G Protein
  2. LPL Receptor

LPL Receptor

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 Related Products (111):

Cat. No. Product Name Effect Purity
  • HY-100619
    BMS-986020 Antagonist 99.53%
    BMS-986020 (AM152) is a high-affinity and selective lysophosphatidic acid receptor 1 (LPA1) antagonist[1]. BMS-986020 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[2]. BMS-986020 has the potential for the treatment of idiopathic pulmonary fibrosis (IPF)[3].
  • HY-19989A
    MK-571 sodium Inhibitor
    MK-571 (L-660711) sodium 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 sodium is also a inhibitor of multidrug resistance-associated protein MRP4 (ABCC4) and ABCC1 (MRP1). MK-571 sodium inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release[1][2][3].
  • HY-12005
    Fingolimod hydrochloride Modulator
    Fingolimod hydrochloride (FTY720), an analog of sphingosine, is a potent sphingosine 1-phosphate (S1P) receptors modulator. Fingolimod hydrochloride is phosphorylated by sphingosine kinases, particularly by SK2, and then binds S1PR1, 3, 4, and 5. Fingolimod hydrochloride induces the internalization of S1P1, and consequently, inhibits S1P activity. Fingolimod hydrochloride also is a pak1 activator[1][4].
  • HY-12288
    Ozanimod Agonist 99.83%
    Ozanimod (RPC-1063), a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity selectively to S1P receptor subtypes 1 (S1P1) and 5 (S1P5). Ozanimod has modulate effect for hS1P1 and hS1P5 receptor with EC50s of 1.03 nM and 8.6 nM, respectively. Ozanimod can be used for the research of relapsing multiple sclerosis (MS)[1].
  • HY-12355
    Siponimod Agonist
    Siponimod (BAF-312) 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[1]-[4].
  • HY-148801
    Tamuzimod Modulator
    Tamuzimod is a potent immunomodulator. Tamuzimod has S1P Receptor modulatory activity with EC50s <1 μM[1][2].
  • HY-149210
    S1PR1 Radioligand 1
    S1PR1 Radioligand 1(compound 6 h) is a specific S1PR1 radioligand with IC50 = 8.7 nM. S1PR1 Radioligand 1 has good brain uptake and can be used as a S1PR1-specific F-18 radiotracer for studying the function of S1PR1 in brain diseases[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[1].
  • HY-18166
    NIBR0213 Antagonist
    NIBR-0213 is a potent and selective S1P1 antagonist with efficacy in experimental autoimmune encephalomyelitis. NIBR-0213 displays potent and comparable potency on human and rat S1P1 (IC50 of 2.0 nM and 2.3 nM, respectively) in GTPγ35S assays[1].
  • HY-108496S
    Sphingosine-1-phosphate-d7 Agonist
    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].
  • 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[1][2].
  • HY-101395A
    W146 TFA Antagonist 98.13%
    W146 TFA is a selective antagonist of sphingosine-1-phosphate receptor 1 (S1PR1) with an EC50 value of 398 nM.
  • 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[1][2].
  • HY-113934
    L-threo Lysosphingomyelin (d18:1) Agonist
    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[1].
  • HY-107615
    TC LPA5 4 Antagonist 99.22%
    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[1]. TC LPA5 4 inhibits cell proliferation and migration of thyroid cancer cells[2].
  • 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[1].
  • HY-17606
    Cenerimod Agonist
    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[1][2].
  • 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).
  • HY-11063S1
    Fingolimod-d4 hydrochloride Antagonist
    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].
  • 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[1].