LPL Receptor Antagonist

LPL Receptor Antagonists (47):

Cat. No.	Product Name	Effect	Purity

HY-11063

Fingolimod	Antagonist	99.97%
Fingolimod (FTY720 free base) is a 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.

HY-100675

JTE-013	Antagonist	99.92%
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.

HY-139853

BMS-986278	Antagonist	99.95%
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.

HY-13285

Ki16425	Antagonist	98.11%
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.

HY-100619

BMS-986020	Antagonist	99.91%
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).

HY-12789

Etrasimod	Antagonist	99.91%
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.

HY-19736

TY-52156	Antagonist	99.42%
TY-52156 is a potent and selective S1P₃ receptor antagonist with a K_i value of 110 nM.

HY-15277

AM966	Antagonist	99.86%
AM966 is a high affinity, selective, oral LPA₁-antagonist, inhibits LPA-stimulated intracellular calcium release (IC₅₀=17 nM).

HY-16039

AM095	Antagonist	99.72%
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.

HY-101395

W146	Antagonist	99.83%
W146 is a selective antagonist of sphingosine-1-phosphate receptor 1 (S1PR1) with an EC₅₀ value of 398 nM.

HY-119401

CAY10444	Antagonist	≥98.0%
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.

HY-101395A

W146 TFA	Antagonist	98.13%
W146 TFA is a selective antagonist of sphingosine-1-phosphate receptor 1 (S1PR1) with an EC₅₀ value of 398 nM.

HY-136462

CYM50358	Antagonist	98.04%
CYM50358 is a potent and selective S1PR4 antagonist, with an IC₅₀ of 25 nM. CYM50358 can be used for the research of influenza infection.

HY-15706

H2L 5765834	Antagonist	98.66%
H2L 5765834 is an antagonist of lysophosphatidic acid receptors LPA₁, LPA₃, and LPA₅, with IC₅₀s of 94, 752, and 463 nM respectively.

HY-156815

YL-365	Antagonist	99.96%
YL-365 is a angonist of GPR34. YL-365 is used for pain and cancer research.

HY-107616

H2L5186303	Antagonist	98.72%
H2L5186303 is an effective and selective LPA₂ receptor antagonist, with an IC₅₀ of 9 nM, and it has anti-inflammatory effects. H2L5186303 can inhibit intestinal cell proliferation and promote apoptosis.

HY-139310

GLPG2938	Antagonist	99.93%
GLPG2938 is a potent and selective S1P2 antagonist. GLPG2938 can be used for the research of idiopathic pulmonary fibrosis.

HY-107615

TC LPA5 4	Antagonist	99.69%
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.

HY-114379

AS2717638	Antagonist	99.53%
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.

HY-18641

Ki16198	Antagonist	98.17%
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.

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