Lysophospholipid
Members of the family of Lysophospholipid receptors are GPCRs (GPCR-A13) that are important for lipid signaling[1]. Their endogenous ligands encompass lysophosphatidic acid (LPA) and sphingosine 1-phosphate (S1P). The principal effects of LPA and S1P are growth related, including induction of cellular proliferation, alterations in differentiation and survival, and suppression of apoptosis. LPA and S1P also evoke cellular effector functions, which are dependent on cytoskeletal responses such as contraction, secretion, adhesion, and chemotaxis[2],[3]. The classical S1PR1 ligand Fingolimod (FTY 720, Axon 1485) is known for its characteristics as an immunomodulating drug, approved for treating multiple sclerosis. Interestingly, recent studies indicated the ligand could also be a candidate therapeutic drug for the treatment of heart failure and arrhythmias by activation of the P21-activated kinase-1 (Pak1)[4].
[1] InternationalUnion of Pharmacology. XXXIV. Lysophospholipid receptor nomenclature.J Chun, EJ Goetzl, T Hla, Y Igarashi, KR Lynch, W Moolenaar, S Pyne, G Tigyi. Pharmacol Rev 2002, 54, 265–269.
[2] Diversity of cellular receptors and functions for the lysophospholipid growth factors lysophosphatidic acid and sphingosine 1-phosphate. EJ Goetzl, S An. FASEB J 1998, 12, 1589-1598.
[3] Lysophospholipid receptors: signaling, pharmacology and regulation by lysophospholipid metabolism. D Meyer zu Heringdorf, KH Jakobs. Biochim. Biophys. Acta 2007, 1768 , 923–940.
[4] FTY720 prevents ischemia/reperfusion injury-associated arrhythmias in an ex vivo rat heart model via activation of Pak1/Akt signaling. EE Egom, Y Ke, H Musa, T Mohamed, T Wang,E Cartqright, RJ Solaro, M Lei. J. Mol. Cell. Cardiol. 2010, 48, 406-414.
| Axon ID | Name | Description | From price | |
|---|---|---|---|---|
| 2367 | AM 095 (parent compound) | Novel potent and selective LPA1 antagonist | €125.00 | |
| 3096 | Amiselimod hydrochloride | S1PR modulator | €105.00 | |
| 3609 | AS2717638 | Highly potent, selective, orally active, and brain-penetrant LPA receptor 5 antagonist | €180.00 | |
| 1485 | Fingolimod | S1PR1 agonist; Immunosuppressant | €60.00 | |
| 1866 | JTE 013 | S1PR2 antagonist | €130.00 | |
| 1615 | KRP203 | S1PR1 agonist | €145.00 | |
| 1947 | RP 001 hydrochloride | A picomolar S1PR1 agonist | €110.00 | |
| 1672 | SEW 2871 | S1PR1 agonist | €80.00 | |
| 2404 | TY 52156 | Selective, competitive, and orally active S1P3 antagonist | €110.00 | |
| 3207 | UCM-05194 ammonium salt | Potent and selective LPA1 receptor agonist | €140.00 | |