LPL Receptor Antagonist

LPL Receptor Antagonists (35):

Cat. No.	Product Name	Effect	Purity

HY-11063

Fingolimod	Antagonist	99.56%
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-W701470

W140 hydrobromide	Antagonist
W140 hydrobromide is a S1P1 antagonist with the K_i of 2.84 μM, and can enhanceof capillary leakage and restoration of lymphocyte egress.

HY-100675

JTE-013	Antagonist	99.57%
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-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-139853

BMS-986278	Antagonist	99.78%
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-12789

Etrasimod	Antagonist	99.82%
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-15277

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

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-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-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-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-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-107615

TC LPA5 4	Antagonist	99.22%
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-107616

H2L5186303	Antagonist	98.72%
H2L5186303 is a potent and selective LPA² receptor (lysophosphatidic acid 2 receptor) antagonist with an IC₅₀ of 9 nM.

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-114379

AS2717638	Antagonist	99.53%
AS2717638 is an oral active and selective lysophosphatidic acid receptor 5 (LPA5) antagonist, with an IC₅₀ of 38 nM for hLPA5. AS2717638 also significantly improves PGE₂-, PGF_2α-, and AMPA-induced allodynia.

HY-15706

H2L 5765834	Antagonist	98.36%
H2L 5765834 is an antagonist of lysophosphatidic acid receptors LPA₁, LPA₃, and LPA₅, with IC₅₀s of 94, 752, and 463 nM respectively.

HY-18641

Ki16198	Antagonist	98.04%
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.

HY-113973

LPA2 antagonist 2	Antagonist
LPA2 antagonist 2 (H2L 5226501) is a selective LPA₂ antagonist with an IC₅₀ of 28.3 nM and a K_i of 21.1 nM. LPA2 antagonist 2 is >480-fold more selective than LPA₃ (IC₅₀ of 13.85 μM).

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