pro-FTY, a FTY720 anticancer prodrug, is a sphingosine-1-phosphate (S1P) inhibitor. pro-FTY specifically inhibits S1P signaling in cancer cells using a drug delivery system (DDS) that reacts with acrolein. pro-FTY significantly inhibits the survival of breast cancer cells, including multidrug-resistant cells and its organoids resistant to Paclitaxel or Doxorubicin. pro-FTY potently suppresses tumor growth in 4T1 cells or organoids xenograft tumors mice model while avoiding lymphocytopenia.

BMT-136088 is a radioligand used for positron emission tomography (PET) imaging of idiopathic pulmonary fibrosis.

1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA is a phospholipid containing arachidonic acid at the sn-1 position. It is a precursor to 1-arachidonoyl glycerol (1-Monoarachidin). 1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA binds to the LPA2/EDG4 receptor with an EC50 value of approximately 10 nM. It prevents TNF-α and IL-6 secretion in wild-type but not Lpa2-/- dendritic cells stimulated by LPS. It also decreases differentiation of HT-29 human colon carcinoma cells to goblet cells in the presence of sodium butyrate.

UCM-05194 (ammonium) is a lysophosphatidic acid receptor 1 (LPA1) agonist. UCM-05194 (ammonium) induces calcium mobilization in LPA1-expressing RH7777 cells (EC50 = 0.24 µM). UCM-05194 (ammonium) induces neurite retraction and migration in LPA1-overexpressing B103 rat neuroblastoma cells. UCM-05194 (ammonium) attenuates acetic acid-induced writhing and hind paw mechanical hypersensitivity in mice.

1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA (sodium) (1-Arachidonoyl-sn-glycerol 3-phosphate (sodium)) is a phospholipid with arachifonic acid at the sn-1 position. 1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA (sodium) binds to the LPA2/EDG4 receptor (EC50 of 10 nM). 1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA (sodium) can be found in rat brain as 37% of the arachidoinic acid-containing lysophosphatidic acid species. 1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA (sodium) is the precursor to 1-arachidonoyl glycerol. 1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA (sodium) can prevent TNF-α and IL-6 secretion in wild type LPS-stimulated dendritic cells. 1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA (sodium) reduces differentiation of HT-29 colon carcinoma cells into goblet cells when sodium butyrate is present.

1-Hexadecyl lysophosphatidic acid (1-Hexadecyl LPA) sodium, an ether analog of lysophosphatidic acid (LPA), is a LPA receptor activator.

GSK1842799 is an orally active selective S1P1 receptor agonist prodrug. GSK1842799 is promising for research of multiple sclerosis.

TRV045 is a selective Sphingosine-1-phosphate subtype 1 receptor agonist with no effect on lymphocyte transport. TRV045 has antiepileptic activity.

KRO-105714 is the antagonist for sphingosine phosphocholine receptor (SPC Receptor) and sphingosine-1-phosphate receptor 1 (S1P1 Receptor) (IC50=79.2 nM). KRO-105714 inhibits SPC-induced proliferation of NIH3T3 (IC50=5.6 nM), inhibits SPC-induced cell migration (IC50=0.59 μM) and tube formation in HUVECs. KRO-105714 inhibits SPC-induced generation of IL-4 and IL-5, exhibits anti-inflammtory efficacy in mouse atopic dermatitis models.

(Rac)-1-Oleoyl lysophosphatidic acid is an isomer of 1-Oleoyl lysophosphatidic acid sodium.

H2L5186303 is a potent and selective LPA2 receptor (lysophosphatidic acid 2 receptor) antagonist with an IC50 of 9 nM.

BMS-986278 is a potent lysophosphatidic acid receptor 1 (LPA1) antagonist, with a human LPA1 Kb of 6.9 nM.

ONO-0740556 is a potent Gi-coupled human lysophosphatidic acid receptor 1 (LPA1) agonist with an EC50 value of 0.26 nM.

Fingolimod phosphate (FTY720 phosphate) is an orally active sphingosine 1-phosphate (S1P) receptor agonist. Fingolimod phosphate can promote the neuroprotective effects of microglia. Fingolimod phosphate can be used for the research of multiple sclerosis and neurologic diseases.

SLF1081851 (16 d) is an effective Sphingolipid Transporter 2 (Spns2) (S1P transporter) inhibitor with an IC50 value of 1.93 μM (S1P), SLF1081851 inhibits SphK2 with an IC50 value of ≈ 30 μM (SphK2), and is at least 15-fold more selective for SphK2 than SphK1. SLF1081851 has the potential to investigate Spns2 biology and can be used for autoimmune encephalomyelitis (EAE) research.

IMMH001, also called SYL930, is an orally active, potent and selective S1P1 (sphingosine-1-phosphate receptor 1) agonist. IMMH001 decreased levels of both chemokines and proinflammatory cytokines, including IL-1β, IL-5, IL-18, IP10, CCL3, and CCL5. IMMH001 can be used for rheumatoid arthritis (RA) research.

CYM50179 (compound 22n) is a potent and selective S1P4-R (Sphingosine-1-phosphate4 receptor) agonist with an EC50 of 46 nM.

TC-SP 14 (compound 14) is an orally active and potent S1P1 agonist (EC50 = 0.042 μM) with minimal activity at S1P3 (EC50 = 3.47 μM). TC-SP 14 significantly reduces blood lymphocyte counts and attenuates a delayed type hypersensitivity (DTH) response to antigen challenge.

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).

A6770 is an orally active, potent sphingosine 1-phosphate (S1P) lyase (S1PL) inhibitor. A6770 is phosphorylated and the phosphorylated form directly inhibits S1P lyased.A6770, a potential key metabolite of THI, induces a [3H]dhS1P increase.

L-threo Lysosphingomyelin (d18:1) (L-threo-Sphingosylphosphorylcholine) is an endogenous bioactive sphingolipid. L-threo Lysosphingomyelin (d18:1) is a potent S1P receptor agonist with EC50s of 19.3, 131.8, and 313.3 nM for hS1P1, hS1P3, and hS1P2, respectively.

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 3 is a selective G-protein-biased sphingosine-1 phosphate receptor-1 (S1P1 ) agonist for endothelial protection.

W146 TFA is a selective antagonist of sphingosine-1-phosphate receptor 1 (S1PR1) with an EC50 value of 398 nM.

S1P2 antagonist 1 is an orally bioavailable S1P2 antagonist against fibrotic diseases.