LPL Receptor

Lysophospholipid (LPL) receptor modulators here act mainly on sphingosine-1-phosphate (S1P) signaling. Lysophospholipid receptors are G protein-coupled receptors for lysophosphatidic acid (LPA) and S1P. A 2010 nomenclature review listed five LPA receptors with a proposed sixth (LPA1 to LPA6) and five S1P receptors. Ceralifimod, S1P1 agonist 1 and (S)-FTY720-phosphonate are agonists at S1P receptor 1, which controls lymphocyte exit from lymphoid organs. Other compounds change the amount of ligand available to the receptors. SLF1081851 and SLF80821178 inhibit spinster homolog 2 (Spns2), a transporter that exports S1P from cells. Spns2 was identified in 2009 as a sphingolipid transporter needed for migration of zebrafish myocardial precursors. S1PL-IN-1 inhibits S1P lyase, the enzyme that degrades S1P irreversibly inside cells.

5 Items

  • S1P1 agonist 4
    Cat. No.
    A61189

    S1P1 agonist 4

    S1P1 agonist 4 is a potent LPL receptor modulator that exhibits high efficacy with an EC50 of less than 0.05 mg/kg. This compound is characterized by a favorable human half-life, approximately 5 days, making it an ideal candidate for studies involving lipid metabolism and cardiovascular disease research. Its ability to selectively activate S1P1 receptors positions it as a valuable tool for exploring therapeutic strategies in metabolic disorders.

    25 mg
    $1,800.00
    50 mg
    $2,285.00
    All 3 sizes
  • GSK 1842799 TFA
    Cat. No.
    A61200

    GSK 1842799 TFA

    GSK 1842799 TFA is a selective modulator of the S1P1 receptor, primarily developed for the treatment of multiple sclerosis (MS). The phosphorylated derivative, GSK1842799-P, demonstrates subnanomolar agonist activity for S1P1, with over 1000-fold selectivity against S1P3. This compound exhibits favorable pharmacokinetics, including good oral bioavailability and rapid in vivo conversion, leading to significant lymphocyte count reduction at a dose of 0.1 mg/kg. In preclinical models, it showcased comparable efficacy to FTY720, supporting its potential utility in MS research and other immune-related conditions.

    25 mg
    $1,655.00
    50 mg
    $2,115.00
    All 3 sizes
  • BMS-986104
    Cat. No.
    A61222

    BMS-986104

    BMS-986104 is a selective modulator of the S1P1 receptor, exhibiting significant biological activity in promoting remyelination. It demonstrates efficacy in a mouse model of experimental autoimmune encephalomyelitis (EAE), showing comparable results to established agents. Mechanistically, BMS-986104 effectively facilitates remyelination in a three-dimensional brain cell culture assay involving lysophosphatidylcholine-induced demyelination, making it a valuable tool for research on neurodegenerative diseases and myelin repair mechanisms.

    Out of stock

    All 3 sizes
  • CS-0777
    Cat. No.
    A61235

    CS-0777

    CS-0777 is a selective sphingosine 1-phosphate receptor-1 modulator that exhibits oral bioavailability. This compound is primarily utilized in research focused on autoimmune diseases, where it influences immune cell trafficking and potentially alters disease progression. Its mechanism of action offers valuable insights into the therapeutic targeting of sphingosine pathways in various pathological conditions.

    Out of stock

    All 3 sizes
  • S1PR1-MO-1
    Cat. No.
    A61257

    S1PR1-MO-1

    S1PR1-MO-1 is a modulator of the sphingosine-1-phosphate receptor (S1PR1) that plays a critical role in various cellular processes. It exhibits significant biological activity in regulating inflammatory responses and hyperproliferative conditions. This reagent is primarily utilized in research focused on understanding and developing therapeutic strategies for inflammatory diseases and related disorders.

    25 mg
    $1,530.00
    50 mg
    $1,950.00
    All 3 sizes

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