LPL Receptor Antagonist

JTE-013 is a potent and specific S1P₂ (Sphingosine-1-Phosphate 2; EDG-5) antagonist. JTE-013 inhibits the specific binding of radiolabeled S1P to human and rat S1P₂ with IC₅₀s of 17 nM and 22 nM, respectively.

Fingolimod (FTY720 free base) is a brain-penetrant 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.

BMS-986278 is a potent and orally active lysophosphatidic acid receptor 1 (LPA1) antagonist, with K_bs of 6.9 nM and 4.0 nM for human and mouse LPA1, respectively. BMS-986278 can be used for the research of pulmonary fibrotic diseases.

Ki16425 (Debio 0719) is a subtype-selective, competitive antagonist of the EDG-family receptors, LPA1 and LPA3 with K_is of 0.34 μM and 0.93 μM, respectively. Ki16425 (Debio 0719) reduces the LPA-induced activation of p42/p44 MAPK. Ki16425 can also inhibit LPA-induced dephosphorylation of Yes-associated protein (YAP)/TAZ in HEK293A cells.

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

TY-52156 is a potent and selective S1P₃ receptor antagonist with a K_i value of 110 nM.

BMS-986020 (AM152) is a high-affinity and selective lysophosphatidic acid receptor 1 (LPA1) antagonist. BMS-986020 inhibits bile acid and phospholipid transporters with IC₅₀s of 4.8 μM, 6.2 μM, and 7.5 μM for BSEP, MRP4, and MDR3, respectively. BMS-986020 has the potential for the treatment of idiopathic pulmonary fibrosis (IPF).

Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P₁) receptor with an IC₅₀ value of 1.88 nM in CHO cells.

AM966 is a high affinity, selective, oral LPA₁-antagonist, inhibits LPA-stimulated intracellular calcium release (IC₅₀=17 nM).

AM095 is a selective LPA₁ receptor antagonist. The IC₅₀ for AM095 antagonism of LPA-induced calcium flux of human or mouse LPA₁-transfected CHO cells is 0.025 and 0.023 μM, respectively.

H2L5186303 is a potent and selective LPA₂ receptor antagonist with an IC₅₀ of 9 nM. H2L5186303 promotes Apoptosis. H2L5186303 inhibits cell proliferation and motility. H2L5186303 has anti-inflammatory effects.

CAY10444 (BML-241) is a sphingosine-1-phosphate 3 (S1P3) antagonist. CAY10444 inhibits by 37% S1P-induced increases in Ca²⁺ in HeLa cells expressing S1P3 receptors.

AS2717638 is a highly selective, brain-penetrant and orally active lysophosphatidic acid receptor 5 (LPA5) antagonist with an IC₅₀ value of 38 nM. AS2717638 is highly selective and shows no significant antagonistic activity against other LPA receptors (LPA1, LPA2, and LPA3). AS2717638 can be used in the research of pain and neuroinflammation-related diseases.

CYM50358 is a potent and selective S1PR4 antagonist, with an IC₅₀ of 25 nM. CYM50358 can be used for the research of influenza infection.

H2L 5765834 is an antagonist of lysophosphatidic acid receptors LPA₁, LPA₃, and LPA₅, with IC₅₀s of 94, 752, and 463 nM respectively.

GLPG2938 is a potent and selective S1P2 antagonist. GLPG2938 can be used for the research of idiopathic pulmonary fibrosis.

TC LPA5 4 is a LPA₅ (GPR92)-specific non-lipid antagonist. TC LPA5 4 inhibits LPA-induced aggregation of isolated human platelet (LPA₅-RH7777 cell line) with an IC₅₀ of 800 nM. TC LPA5 4 displays selectivity for LPA₅ over 80 other screened agent targets. TC LPA5 4 inhibits cell proliferation and migration of thyroid cancer cells.

NIBR-0213 is a potent, orally active and selective S1P1 antagonist with efficacy in experimental autoimmune encephalomyelitis. NIBR-0213 displays potent and comparable potency on human and rat S1P1 (IC₅₀ of 2.0 nM and 2.3 nM, respectively) in GTPγ³⁵S assays.

ACT-1016-0707 (Compound 49) is an orally active and selective LPA1 receptor antagonist. ACT-1016-0707 can be used for the research of fibrotic diseases.

ONO-7300243 is a novel, potent lysophosphatidic acid receptor 1 (LPA1) antagonist with IC₅₀ of 0.16 μM.