2. Signaling Pathways
  3. GPCR/G Protein
  4. LPL Receptor

LPL Receptor

Lysophospholipid Receptor

LPL Receptor

Related Products

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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-119245
    Udifitimod
    		Modulator
    Udifitimod (BMS-986166) is a potent, selective and orally active S1P1R modulator. Udifitimod has the potential for the research of autoimmune diseases.
    Udifitimod
  • HY-125046
    CYM50374
    		Antagonist
    CYM50374 is a potent antagonist sphingosine-1-phosphate 4 (S1P4) antagonists, with the IC50 of 34 nM.
    CYM50374
  • HY-P991311
    GSK3178022
    		Inhibitor
    GSK3178022 is a human IgG1 monoclonal antibody (mAb) targeting LRP6. GSK3178022 inhibits the expression of WNT target genes SP5 and AXIN2. GSK3178022 has antitumor activity in the RSPO fusion model of colorectal cancer. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001).
    GSK3178022
  • HY-16622A
    GSK 1842799 TFA
    		Modulator
    GSK1842799, an alkyl-substituted biaryl amino alcohol, is a selective S1P1 modulator developed for multiple sclerosis (MS). Upon phosphorylation, GSK1842799-P exhibited subnanomolar S1P1 agonist activity with over 1000-fold selectivity over S1P3. The compound showed good oral bioavailability, rapid in vivo conversion to GSK1842799-P, and significant lymphocyte count reduction at 0.1 mg/kg. It matched FTY720 efficacy at 3 mg/kg in the mouse EAE model and achieved comparable plasma levels to FTY-720 phosphate in cynomolgus monkeys. With favorable ADME, PK/PD properties, and toxicology, GSK1842799 advanced to further clinical development.
    GSK 1842799 TFA
  • HY-142032
    RBM10-8
    		Inhibitor
    RBM10-8 is irreversible inhibitor of recombinant  human sphingosine-1-phosphate lyase (hS1PL) . Sphingosine-1-phosphate (S1P) is a sphingolipid (SL) that acts as a signaling molecule regulating diverse cellular processes such as cell proliferation and differentiation, angiogenesis, immune function, inflammation, and development.
    RBM10-8
  • HY-101939
    RP-001
    		Agonist
    RP-001 is a picomolar short-acting S1P1 (EDG1) selective agonist, with an EC50 of 9 pM. RP-00 induces internalization and polyubiquitination of S1P1. RP-001 has little activity on S1P2-S1P4 and only moderate affinity for S1P5.
    RP-001
  • HY-120468
    GSK2263167
    		Agonist
    GSK2263167 is a S1P1 receptor agonist
    GSK2263167
  • HY-14977
    CS-0777-P
    		Agonist
    CS-0777-P, the phosphorylated form of CS-0777, acts as a potent and selective modulator of the S1P receptor-1 (S1P1). It exhibits approximately 320-fold higher agonist activity for human S1P1 compared to S1P3, with an EC50 of 1.1 nM. In pharmacological studies, CS-0777-P demonstrated significant effects in vitro as an S1P1 and S1P3 agonist, leading to lowered peripheral blood lymphocyte counts and suppressive effects on experimental autoimmune encephalomyelitis (EAE) in rats. Pharmacokinetic studies in rats revealed rapid lymphocyte count reductions following oral administration, making CS-0777 a promising candidate currently undergoing clinical trials for the treatment of multiple sclerosis (MS).
    CS-0777-P
  • HY-114061
    (R)-FTY 720P
    		Inhibitor
    (R)-FTY 720P is the R-isomer of FTY 720P. (R)-FTY 720P has less potent binding affinities to S1P1,3,4,5 than (S)-Isomer (HY-15382).
    (R)-FTY 720P
  • HY-173324
    LPA2 antagonist 5
    		Antagonist
    LPA2 antagonist 5 (EX1) is a LPA2 antagonist, with an IC50 of 4.05 nM.
    LPA2 antagonist 5
  • HY-160616
    LPA5 antagonist 3
    		Antagonist
    LPA5 antagonist 3 (Example 74) is a lysophosphatidic acid receptor 5 (LPA5) antagonist, with an IC50 of 170 nM. LPA5 antagonist 3 can be used for the research of pain disorders and atherosclerosis.
    LPA5 antagonist 3
  • HY-124072
    HL001
    		Antagonist
    HL001 is an orally active small molecule inhibitor of Cyclophilin A (CypA) and a receptor antagonist of Lysophosphatidic acid 1 (LPA1). HL001 induces cell cycle arrest and apoptosis of tumor cells by p53. HL001 stabilizes p53 by down-regulating G3BP1, inducing reactive oxygen species and DNA damage. HL001 disrupts the interaction between MDM2 and p53-72R in a CypA dependent manner. HL001 has antitumor activity. HL001 can also be used to study pulmonary fibrosis.
    HL001
  • HY-118919
    CYM5181
    		Agonist
    CYM5181 is a novel S1P1 agonist with a pEC50 value of -8.47.
    CYM5181
  • HY-W779969
    2-Acetyl-4-tetrahydroxybutyl imidazole-13C6
    2-Acetyl-4-tetrahydroxybutyl imidazole-13C6 is the 13C-labeled 2-Acetyl-4-tetrahydroxybutyl imidazole (HY-14113). 2-Acetyl-5-tetrahydroxybutyl imidazole is a potent sphingosine-1-phosphate (S1P) lyase inhibitor in vivo.
    2-Acetyl-4-tetrahydroxybutyl imidazole-<sup>13</sup>C<sub>6</sub>
  • HY-RS12401
    S1pr4 Mouse Pre-designed siRNA Set A
    		Inhibitor

    S1pr4 Mouse Pre-designed siRNA Set A contains three designed siRNAs for S1pr4 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    S1pr4 Mouse Pre-designed siRNA Set A
  • HY-148292
    C16-Sphingosine-1-phosphate
    C16-Sphingosine-1-phosphate is a derivative of Sphingosine-1-phosphate and also an endogenous ligand for the EDG/S1P receptor. C16-Sphingosine-1-phosphate can be used in the research of angiogenesis, inflammation, and cardiovascular diseases.
    C16-Sphingosine-1-phosphate
  • HY-119221A
    AUY 954 hydrochloride
    		Agonist
    AUY 954 hydrochloride is a potent and selective sphingosine-1-phosphate (S1P(1)) receptor agonist, exhibiting significant immunomodulatory activity. AUY 954 hydrochloride induces a profound and reversible reduction of circulating lymphocytes upon oral administration. AUY 954 hydrochloride has demonstrated efficacy in prolonging cardiac allograft survival when used in combination with RAD001 in a stringent transplantation model. AUY 954 hydrochloride effectively prevents experimental autoimmune neuritis in rats, showcasing its therapeutic potential in autoimmune conditions.
    AUY 954 hydrochloride
  • HY-120611
    BMS-960 free base
    		Agonist
    BMS-960 free base is a potent and selective S1P1 receptor agonist containing isoxazole, which can be used in the research of immune diseases and vascular diseases.
    BMS-960 free base
  • HY-156565
    S1P1 agonist 6
    		Agonist
    S1P1 agonist 6 (Compound I) is a S1P1 agonist that reduces autoimmune ability by blocking the transportation of lymphocytes. S1P1 agonist 6 can be used as an immunosuppressive agent in the study of various autoimmune diseases research.
    S1P1 agonist 6
  • HY-129808
    VPC12249
    		Antagonist
    VPC12249 is a competitive dual LPA1/LPA3 antagonist with Ki values of 137nM and 428 nM, respectively. VPC12249 inhibits calcium mobilization in HEK293T cells with a Ki value of ~130 nM. VPC12249 is promising for research of ovarian cancer and hypertensive diseases.
    VPC12249
Cat. No. Product Name / Synonyms Application Reactivity
LPL Receptor Isoform Comparison

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