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S1P Receptor

The sphingosine-1-phosphate receptors are a class of G protein-coupled receptors that are targets of the lipid signalling molecule Sphingosine-1-phosphate (S1P). They are divided into five subtypes: S1PR1, S1PR2, S1PR3, S1PR4 and S1PR5. .

Phorbol 12-myristate 13-acetate
TQ019816561-29-8
Phorbol 12-myristate 13-acetate (PMA), a member of the phorbol ester group of natural products, activates PKC, SphK, and NF-κB, and induces THP1 cell differentiation.
  • $44
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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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SKI-178
T90141259484-97-3
SKI-178 is a sphingosine kinase 1 (SphK1) inhibitor with IC50 of 0.1-1.8 μM. It induces prolonged mitosis followed by apoptotic cell death through the intrinsic apoptotic cascade. The sustained activation of CDK1 during prolonged mitosis, mediated by SKI-178 leads to the simultaneous phosphorylation of the prosurvival Bcl-2 family members, Bcl-2 and Bcl-xl, as well as the phosphorylation and subsequent degradation of Mcl-1.
  • $41
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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).
  • $48
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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.
  • $46
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Opaganib
T6750915385-81-8
Opaganib (ABC294640) is an orally active and specific sphingosine kinase-2 (SphK2) inhibitor (IC50: 60 μM).
  • $34
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GLPG2938
T91992130996-00-6
GLPG2938 (1-(2-Ethoxy-6-(trifluoromethyl)pyridin-4-yl)-3-((5-methyl-6-(1-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl)pyridazin-3-yl)methyl)urea) is a potent and selective antagonist of S1P2.
  • $76
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SAR-114137
T28658537706-31-3In house
SAR-114137 is a histone sphingomyelin kinase inhibitor used in the study of molluscum arteriosum and peripheral neuropathic pain.
  • $490
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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.
  • $33
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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).
  • $35
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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.
  • $41
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LX-2931
T27864948840-25-3In house
LX-2931(LX-3305) is a sphingosine-1-phosphate cleavage enzyme (S1P) inhibitor for the treatment of rheumatoid arthritis.
  • $258
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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).
  • $70
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K6PC-5
T27710756875-51-1
K6PC-5 is a ceramide derivative that acts as an activator of sphingosine kinase 1 (SPHK1), inducing a swift and temporary rise in intracellular calcium levels. With its potential applications in skin diseases associated with abnormal keratinocyte function, as well as in studies on neurodegeneration and virus infection, K6PC-5 presents a promising compound for research purposes.
  • $34
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W140 HBr
T602041246817-25-3In house
[(3S)-3-amino-4-(3-hexylanilino)-4-oxobutyl]phosphonic acid;hydrobromide is a S1P1 antagonist with Ki of 2.84 μM.
  • $117
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AMG-369
T299711202073-26-4In house
AMG-369 (AMG 247) is an S1P1 S1P5 dual agonist that delays the onset of experimental autoimmune encephalomyelitis in rats. encephalomyelitis in rats.
  • $413
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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).
  • $30
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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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CYM-5520
T227031449747-00-5
CYM-5520 is a noncompetitive allosteric agonist of S1P2
  • $40
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SKI II
T6673312636-16-1
SKI II (SphK-I2) is a highly selective and non-ATP-competitive S1P receptor inhibitor (IC50: 0.5 μM) while exhibiting no inhibitory action on other kinases including PKCα, PI3K, and ERK2.
  • $34
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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.
  • $38
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BMS-960
T268661265321-86-5In house
BMS-960 is an S1P agonist with potential anti-tumour activity for cancer research.
  • $749
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SEW​2871
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.
  • $48
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SK1-IN-1
T129271218816-71-7
SK1-IN-1 is an orally available and potent sphingosine kinase 1 (SPHK1) inhibitor (IC50: 58 nM), with potential anticancer activity, and can be used to study cancer and neurodegenerative diseases.
  • $216
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