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.

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.

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).

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.

ASP6432 is a potent and selective type 1 lysophosphatidic acid receptor (LPA1) antagonist with IC₅₀s of 11 nM and 30 nM for human LPA1 and rat LPA1, respectively.

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

GS-2278 is an LPAR1 (lysophosphatidic acid receptor 1) antagonist with potential for research in idiopathic pulmonary fibrosis (IPF).

Fingolimod (Standard) is the analytical standard of Fingolimod. This product is intended for research and analytical applications. 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.

Ki16198 is a potent and orally active LPA receptor antagonist, the methyl ester of Ki16425 (HY-13285). Ki16198 inhibits LPA₁ and LPA₃-induced inositol phosphate production with?K_i?values of 0.34 μM and 0.93 μM, respectively. Ki16198 is effective for pancreatic cancer tumorigenesis and metastasis in vivo.

LPA1 receptor antagonist 1 is a highly selective Lysophosphatidic Acid receptor-1 (LPA1) antagonist with an IC₅₀ of 25 nM.

Ex26 (S1P1-IN-Ex26) is a potent and selective sphingosine 1-phosphate receptor 1 (S1P₁) antagonist (IC₅₀=0.93 nM). Ex26 shows >3,000-fold selectivity for S1P₁ over other Sphingosine 1-phosphate receptors. Ex26 can be used in experimental autoimmune encephalomyelitis reseach.

LPAR1 antagonist 1 (compound 18) is a potent, oral active and selective LPAR1 antagonist with the IC₅₀ of 3.3 nM. LPAR1 antagonist 1 can be used for study of fibrosis.

TASP0277308 is a highly selective S1P₁ antagonist. TASP0277308 possesses immunomodulatory activities, including lymphopenia, a block in T cell egress from the thymus, marginal zone B cell displacement, and the upregulation of CD69 expression on lymphocytes. TASP0277308 can be used for the research of collagen-induced arthritis in mice.