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

  • LPA2 antagonist 6
    Cat. No.
    A61191

    LPA2 antagonist 6

    LPA2 antagonist 6 is a potent antagonist targeting lipoprotein(a) [Lp(a)]. It effectively inhibits Lp(a) formation with an IC50 value of 2.33 nM. This compound is instrumental in cardiovascular disease research, allowing for deeper exploration into the mechanisms of lipoprotein metabolism and its role in associated pathologies.

    Out of stock

    All 3 sizes
  • S1P2 antagonist 1
    Cat. No.
    A61243

    S1P2 antagonist 1

    S1P2 antagonist 1 is a potent oral antagonist of the sphingosine-1-phosphate receptor 2 (S1P2). It demonstrates significant biological activity in inhibiting pathways associated with fibrotic diseases. This compound is suitable for research applications exploring the modulation of fibrogenesis and related pathological conditions.

    5 mg
    $795.00
    All 1 sizes
  • (R)-VPC44116
    Cat. No.
    A61246

    (R)-VPC44116

    (R)-VPC44116 is a selective antagonist of the sphingosine-1-phosphate receptor 1 (S1P1). This compound is primarily utilized in lipid signaling research and plays a crucial role in studying immune response, cell migration, and vascular development. Its ability to modulate S1P1 activity makes it valuable for investigating various pathophysiological conditions, including autoimmune diseases and cardiovascular disorders.

    Out of stock

    All 3 sizes
  • KRO-105714
    Cat. No.
    A61248

    KRO-105714

    KRO-105714 is a selective antagonist of the sphingosine phosphocholine receptor (SPC Receptor) and the sphingosine-1-phosphate receptor 1 (S1P1 Receptor), with an IC50 of 79.2 nM. This compound effectively inhibits SPC-induced cell proliferation in NIH3T3 cells (IC50 = 5.6 nM), as well as SPC-induced cell migration (IC50 = 0.59 μM) and tube formation in human umbilical vein endothelial cells (HUVECs). Additionally, KRO-105714 suppresses the generation of pro-inflammatory cytokines IL-4 and IL-5, demonstrating its potential for use in anti-inflammatory research, particularly in mouse models of atopic dermatitis.

    Out of stock

    All 3 sizes
  • VPC 01091
    Cat. No.
    A61252

    VPC 01091

    VPC 01091 is a selective antagonist of the sphingosine-1-phosphate receptor 3 (S1PR3). This compound effectively inhibits S1PR3-mediated signaling pathways, which are implicated in various physiological processes including immune regulation and vascular dynamics. VPC 01091 serves as a valuable tool for research applications aimed at exploring the role of S1PR3 in pathophysiology and therapeutic interventions.

    Out of stock

    All 3 sizes

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