LPL Receptor
Lysophospholipid 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 Isoform Specific Products
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LPL Receptor Inhibitors
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LPL Receptor Agonists
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LPL Receptor Antagonists
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LPL Receptor Activators
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LPL Receptor Modulators
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LPL Receptor Control
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LPL Receptor Ligand
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LPL Receptor Related Products (278)
Related Products (278)
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Antibodies (7)
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LPL Receptor Isoform Comparison
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Udifitimod
0 ImagesCat. No.: HY-119245CAS No.: 1883345-06-9Synonyms: BMS-986166Udifitimod (BMS-986166) is a potent, selective and orally active S1P1R modulator. Udifitimod has the potential for the research of autoimmune diseases.
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CYM50374
0 ImagesCat. No.: HY-125046CAS No.: 1314212-81-1CYM50374 is a potent antagonist sphingosine-1-phosphate 4 (S1P4) antagonists, with the IC50 of 34 nM.
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GSK3178022
0 ImagesCat. No.: HY-P991311GSK3178022 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).
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GSK 1842799 TFA
0 ImagesCat. No.: HY-16622ACAS No.: 1005407-76-0GSK1842799, 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.
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RBM10-8
0 ImagesCat. No.: HY-142032CAS No.: 2407372-42-1RBM10-8 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.
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RP-001
0 ImagesCat. No.: HY-101939CAS No.: 1306761-53-4RP-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.
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GSK2263167
0 ImagesCat. No.: HY-120468CAS No.: 1165924-28-6GSK2263167 is a S1P1 receptor agonist
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CS-0777-P
0 ImagesCat. No.: HY-14977CAS No.: 840523-39-9CS-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).
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(R)-FTY 720P
0 ImagesCat. No.: HY-114061CAS No.: 402616-23-3(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).
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S1P5 receptor agonist-1
0 ImagesCat. No.: HY-148198CAS No.: 2373330-78-8S1P5 receptor agonist-1 (Example 6) is an effective and selective S1P5 receptor (S1P5 receptor) agonist. The EC50 values for S1P5 and S1P1 receptors are 20 nM and > 3 μM, respectively. S1P5 receptor agonist-1 can be used in studies on neuroprotection and immune regulation.
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LPA2 antagonist 5
0 ImagesCat. No.: HY-173324CAS No.: 3070072-52-2LPA2 antagonist 5 (EX1) is a LPA2 antagonist, with an IC50 of 4.05 nM.
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1-Oleoyl lysophosphatidic acid sodium (GMP)
0 ImagesCat. No.: HY-107614GCAS No.: 325465-93-8Synonyms: 1-Oleoyl-sn-glycero-3-phosphate sodium (GMP); 1-Oleoyl-LPA sodium (GMP)1-Oleoyl lysophosphatidic acid sodium (GMP) is the GMP-grade form of 1-Oleoyl lysophosphatidic acid sodium (HY-107614). GMP-grade small molecules serve as auxiliary reagents in cell therapy. 1-Oleoyl lysophosphatidic acid sodium is a bioactive lipid signaling molecule. 1-Oleoyl lysophosphatidic acid sodium inhibits lysoPLD-catalyzed hydrolysis of lysophosphatidylcholine and FS-3. 1-Oleoyl lysophosphatidic acid sodium activates LPA1 and LPA2, thereby triggering calcium mobilization, NFATc1 translocation, Rho/ROCK activation, Smad2/3 phosphorylation and c-Fos expression. 1-Oleoyl lysophosphatidic acid sodium induces anxiety-like, depression-like and hypoactivity phenotypes, regulates osteoclast cytoskeleton and viability, reduces osteoclast bone resorptive activity, and drives mesenchymal stem cell differentiation into myofibroblast-like cells. 1-Oleoyl lysophosphatidic acid sodium stimulates the secretion of transforming growth factor-β1 and stromal cell-derived factor-1. 1-Oleoyl lysophosphatidic acid sodium is applicable to research related to anxiety, depression and ovarian cancer.
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LPA5 antagonist 3
0 ImagesCat. No.: HY-160616CAS No.: 1664336-44-0LPA5 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.
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CYM5181
0 ImagesCat. No.: HY-118919CAS No.: 695155-81-8CYM5181 is a novel S1P1 agonist with a pEC50 value of -8.47.
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Obicetrapib potassium
0 ImagesCat. No.: HY-18778BCAS No.: 866399-90-8Synonyms: TA-8995 potassium; DEZ-001 potassium; AMG-899 potassiumObicetrapib (TA-8995; DEZ-001) potassium is an orally active cholesteryl ester transfer protein (CETP) inhibitor. Obicetrapib potassium potently reduces atherogenic lipoproteins (such as LDL-C, ApoB, Lp (a)) and increases HDL-C. Obicetrapib potassium can be used for the research of dyslipidemia and atherosclerotic cardiovascular disease (ASCVD).
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2-Acetyl-4-tetrahydroxybutyl imidazole-13C6
0 ImagesCat. No.: HY-W779969CAS No.: 1448358-08-42-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.
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VPC 23153
0 ImagesCat. No.: HY-W040167CAS No.: 787582-98-3VPC 23153 is a S1P4 receptor agonist and vasoconstrictor. VPC 23153 activates the S1P4 receptor, thereby triggering vasoconstriction. VPC 23153 induces pulmonary artery contraction. VPC 23153 can be used in studies related to pulmonary arterial hypertension.
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AMG 369
0 ImagesCat. No.: HY-14402CAS No.: 1202073-26-4AMG 369 is an orally active and potent dual S1P1/S1P5 agonist with limited activity at S1P3 and no activity at S1P2/S1P4. AMG 369 reduces blood lymphocyte counts. AMG 369 delays onset and reduces severity of experimental autoimmune encephalomyelitis in rat.
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AUY 954 hydrochloride
0 ImagesCat. No.: HY-119221ACAS No.: 820240-78-6AUY 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.
