LPL Receptor Antagonist

LPL Receptor Antagonists (30):

Cat. No.	Product Name	Effect	Purity

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-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-139853

BMS-986278	Antagonist	99.93%
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-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-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-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-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-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-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-100882

ONO-7300243	Antagonist	98.46%
ONO-7300243 is a novel, potent lysophosphatidic acid receptor 1 (LPA1) antagonist with IC₅₀ of 0.16 μM.

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).

HY-120478

ASP6432	Antagonist
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.

HY-18166

NIBR0213	Antagonist	99.38%
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.

HY-11063S1

Fingolimod-d₄ hydrochloride	Antagonist	≥99.0%
Fingolimod-d₄ (hydrochloride) is the deuterium labeled Fingolimod hydrochloride. Fingolimod hydrochloride (FTY720) is a sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod hydrochloride (FTY720) also is a pak1 activator, a immunosuppressant[1].

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-11063S

Fingolimod-d₄	Antagonist	98.97%
Fingolimod-d₄ is the deuterium labeled Fingolimod. 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[1].

HY-125046

CYM50374	Antagonist
CYM50374 is a potent antagonist sphingosine-1-phosphate 4 (S1P4) antagonists, with the IC₅₀ of 34 nM.

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