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GPCR/G Protein

Cholecystokinin Receptor

Melanin-concentrating Hormone Receptor (MCHR)

(11)

Melanocortin Receptor

Neuropeptide Y Receptor

Prostaglandin Receptor

(199)

Protease-activated Receptor

LPL Receptor

The lysophospholipid receptor (LPL-R) group are members of the G protein-coupled receptor family of integral membrane proteins that are important for lipid signaling. In humans, there are eight LPL receptors, each encoded by a separate gene. These LPL receptor genes are also sometimes referred to as "Edg" (an acronym for endothelial differentiation gene).

Filter HomeSignaling PathwaysGPCR/G ProteinLPL Receptor

Sphingosine-1-phosphate

T2150026993-30-6

Sphingosine-1-phosphate (S1P) is an agonist for S1P1-5 receptors and a ligand for GPR3, GPR6, and GPR12. As an intracellular second messenger, it mobilizes Ca2+ and acts as an extracellular ligand for G-protein coupled receptors. This important lipid mediator is generated from sphingosine or other membrane phospholipids.

$198

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Etrasimod

TQ02271206123-37-6

Etrasimod (APD334) is a specific and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor (IC50: 1.88 nM in CHO cells).

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Ozanimod

T69231306760-87-1

Ozanimod (RPC-1063) (RPC1063) is a specific oral S1P Receptor 1 modulator. Ozanimod has been used in trials studying the treatment of Crohn's Disease, Ulcerative Colitis, Multiple Sclerosis, and Relapsing Multiple Sclerosis.

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PF-543

T60851415562-82-1

PF-543 (Sphingosine Kinase 1 Inhibitor II), a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 of 2.0 nM and Ki of 3.6 nM.

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Siponimod

T64031230487-00-9

BAF312 (Siponimod (BAF-312)), a next-generation S1P receptor modulator, is specific for S1P1 and S1P5 receptors with EC50 of 0.39 nM and 0.98 nM, respectively. The specificity of BAF312 for S1P1 and S1P5 receptors exhibits >1000-fold over S1P2, S1P3 and S1P4 receptors.

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JTE-013

T15629383150-41-2

JTE-013 is an effective and specific antagonist of S1P2. JTE-013 suppresses the specific binding of radiolabeled S1P to human and rat S1P2 (IC50s: 17 nM and 22 nM, respectively).

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SLP9101555

T63047 In house

SLP9101555 is a potent and selective sphingosine kinase 2 (SphK2) inhibitor with a Ki of 90 nM.SLP9101555 has a high affinity for SphK2, which is 200-fold higher than that of SphK1.SLP9101555 dramatically reduces extracellular S1P sphingosine 1-phosphate (S1P) levels.

$350

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S1PR1 modulator 1

T128212328109-05-1In house

S1PR1 modulator 1 is a selective inhibitor of S1PR1, with a pIC50 of 7.6.

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Fingolimod

T7939162359-55-9

Fingolimod (FTY-720A) is an antagonist of sphingosine 1-phosphate (S1P) (IC50 of 0.033 nM in K562 and NK cells).

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Fingolimod hydrochloride

T2539162359-56-0

Fingolimod hydrochloride (FTY720) , a novel immune modulator, is a sphingosine 1-phosphate (S1P) antagonist (IC50: 0.033 nM in K562 and NK cells).

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CYM-5520

T227031449747-00-5

CYM-5520 is a noncompetitive allosteric agonist of S1P2

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Ponesimod

T3258854107-55-4

Ponesimod (ACT-128800) is an orally available sphingosine-1-phosphate receptor 1 (S1PR1, S1P1) agonist with potential immunomodulating activity.

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SEW2871

T2171256414-75-2

SEW 2871 is an orally available, highly selective S1P1 agonist with an EC50 of 13.8 nM.It reduces the number of lymphocytes in the blood and is used in studies related to diabetes, Alzheimer's disease, liver fibrosis, and inflammation. It activates ERK, Akt and Rac signaling pathways and induces S1P1 internalization and recycling.

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Mocravimod hydrochloride

T12086509088-69-1

Mocravimod hydrochloride (KRP-203) is an effecitive and orally active agonist of sphingosine 1-phosphate receptor type 1(S1PR1).

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W146

T13327909725-61-7

W146 is a selective and potent Sphingosine 1-phosphate receptor subtype 1 (S1PR1) antagonist that induces significant but transient hematolymphopenia in mice.W146 induces significant but transient hematolymphopenia in mice, inducing pulmonary edema.

$113

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CYM50260

T150311355026-60-6In house

CYM50260 is a potent and highly selective agonist of the sphingosine-1-phosphate 4 receptor (S1P4-R, EC50= nM), exhibiting no activity against S1P1-R, S1P2-R, S1P3-R, and S1P5-R.

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NIBR-0213

T281691233332-14-3

NIBR-0213 is a potent and selective competitive S1P1 antagonist with activity against experimental autoimmune encephalomyelitis. In the GTPγ35S assay, it has IC50 values of 2.0 nM and 2.3 nM for human and rat S1P1, respectively.

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Ki16425

T6108355025-24-0

Ki16425 (Debio 0719) is a competitive, potent, and reversible antagonist to LPA1, LPA2, and LPA3, with Ki values of 0.34 μM, 6.5 μM, and 0.93 μM, respectively.

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Tyloxapol

T030725301-02-4

Tyloxapol (Triton WR1339) is a non-ionic liquid polymer utilized as a surfactant.

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Sonepcizumab

T768281031360-18-5

Sonepcizumab (LT 1009) is a fully humanized monoclonal antibody against S1P, with anti-cancer activity, useful for studying metastatic renal cell carcinoma (mRCC) and preventing eye scarring after glaucoma filtration surgery.