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-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).
    S1P1 agonist 4
  • HY-156408
    Spns2-IN-1
    		Inhibitor
    Spns2-IN-1 is a potent inhibitor of Spns2-dependent S1P transport (Spns2), with IC50 of 1.4±0.3 μM that plays an important role in immune response.
    Spns2-IN-1
  • HY-12355S
    Siponimod-d11
    		Modulator
    Siponimod-d11 is deuterium labeled Siponimod (HY-12355). Siponimod 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.
    Siponimod-d<sub>11</sub>
  • HY-W701470
    W140 hydrobromide
    		Antagonist
    W140 hydrobromide is a S1P1 antagonist with the Ki of 2.84 μM, and can enhanceof capillary leakage and restoration of lymphocyte egress.
    W140 hydrobromide
  • HY-144126
    S1P1 agonist 5
    		Agonist
    S1P1 agonist 5 is a selective and orally active S1P1 agonist. S1P1 agonist 5 inhibits the lymphocyte egress from the lymphoid tissue to the peripheral blood. S1P1 agonist 5 has the potential for the research of multiple sclerosis (MS).
    S1P1 agonist 5
  • HY-11063S
    Fingolimod-d4
    		Antagonist 98.97%
    Fingolimod-d4 is the deuterium labeled Fingolimod. Fingolimod (FTY720 free base) is a sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator, a immunosuppressant[1].
    Fingolimod-d<sub>4</sub>
  • 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-111292
    CYM-5482
    		Agonist
    CYM-5482 is a potent and selective agonist Sphingosine 1-phosphate receptor 2 (S1PR2) with an IC50 and EC50 of 1.0 and 1.03 μM. CYM-5482 has the potential for the research of cancer diseases.
    CYM-5482
  • 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-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-118919
    CYM5181
    		Agonist
    CYM5181 is a novel S1P1 agonist with a pEC50 value of -8.47.
    CYM5181
  • HY-148801
    Tamuzimod
    		Modulator
    Tamuzimod is a potent immunomodulator. Tamuzimod has S1P Receptor modulatory activity with EC50s <1 μM.
    Tamuzimod
  • 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.
    S1PR1 Radioligand 1
  • 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-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
Cat. No. Product Name / Synonyms Application Reactivity
LPL Receptor Isoform Comparison

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