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GPCR/G Protein S1P Receptor

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. .
Cat No. product name
T10305 Amiselimod hydrochloride Amiselimod hydrochloride is a sphingosine 1-phosphate receptor-1 (S1P1) modulator.
T10385 ASP-4058 ASP-4058 is a selective and oral bioactive agonist for S1P1 and S1P5. It ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety pr...
T11747 KD-3010 KD-3010 is a orally, potent active, and selective PPARδ agonist.
T12436 PF-543 Citrate PF-543 Citrate is an inhibitor of sphingosine-competitive SPHK1(IC50 of 2 nM ).
T12437 PF429242 dihydrochloride PF429242 dihydrochloride is a reversible and competitive inhibitor of S1P (IC50 of 175 nM).
T12927 SK1-IN-1 SK1-IN-1 is a potent inhibitor of sphingosine kinase 1 (SPHK1)(IC50 of 58 nM).
T15032 CYM50308 CYM50308 is a high affinity agonist of sphingosine-1-phosphate receptor 4 (S1P4-R) (EC50: 56 nM). CYM50308 has no activity at S1P1-R, S1P2-R and S1P3-R subtypes...
T17183 TY-52156 TY-52156 is an effective and selective S1P3 receptor antagonist (Ki: 110 nM).
T17237 VPC 23019 VPC 23019 is a competitive antagonist at the S1P1 and S1P3 receptors (pKi= 7.86 and 5.93, respectively). It is also an agonist at the S1P4 and S1P5 receptors (p...
T2026 CYM5442 CYM5442 is an S1P agonist, targeting to Sphingosine.
T2171 SEW2871 Sphingosine-1-phosphate receptor 1 agonist SEW2871 prolongs heterotopic heart allograft survival in mice.
T22703 CYM 5520 noncompetitive allosteric agonist of S1P2
T2539 Fingolimod hydrochlorideHOT Fingolimod, a novel immune modulator, is a sphingosine 1-phosphate (S1P) antagonist (IC50: 0.033 nM in K562 and NK cells).
T3258 Ponesimod Ponesimod is an orally available sphingosine-1-phosphate receptor 1 (S1PR1, S1P1) agonist that acts as a functional antagonist, with potential immunomodulating ...
T3961 CYM 5541 CYM-5541 is a selective and allosteric S1P3 receptor agonist.
T4031 S1p-receptor-agonist-1 An S1P receptor agonist.
T4658 MHP MHP is an activator of sphingosine kinase (SPHK1), and significantly stimulates CAMP mRNA and protein production in KC.
T6085 PF543 PF-543, a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 and Ki of 2.0 nM and 3.6 nM.
T6403 Siponimod BAF312 (Siponimod), 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 specif...
T6673 SKI II SKI II is a highly selective and non-ATP-competitive S1P receptor inhibitor (IC50: 0.5 μM) while exhibiting no inhibitory action on other kinases including PKC...
T6750 ABC294640 ABC294640 is an orally active and specific sphingosine kinase-2 (SphK2) inhibitor (IC50: 60 μM).
T6923 Ozanimod Ozanimod (RPC1063) is a specific oral S1P Receptor 1 modulator. Ozanimod has been used in trials studying the treatment of Crohn's Disease, Ulcerative Colitis, ...
T7360 GSK2018682 GSK2018682 is an agonist of sphingosine-1-phosphate receptor  (s1p1) and (s1p5) agonist(pEC50s of 7.7 and 7.2,respectively).
T7939 Fingolimod Fingolimod is an antagonist of sphingosine 1-phosphate (S1P) (IC50 of 0.033 nM in K562 and NK cells).
T8461 SKI V SKI V is a potent and noncompetitive non-lipid sphingosine kinase (SPHK; SK) inhibitor (GST-hSK,IC50 : 2 μM), and is a PI3K inhibitor(hPI3k,IC50 : 6 μM), indu...
T8840 PF-543 PF-543 inhibits SphK1 with a K(i) of 3.6 nM, is sphingosine-competitive and is more than 100-fold selective for SphK1 over the SphK2 isoform.
T9014 SKI-178 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 intrins...
TQ0138 K145 hydrochloride K145 is a specific inhibitor of SphK2 (IC50: 4.30 μM), while no inhibition of SphK1 at concentrations up to 10 μM.
TQ0198 Phorbol 12-myristate 13-acetate Phorbol 12-myristate 13-acetate (PMA) is a dual SphK and PKC activator.
TQ0227 Etrasimod Etrasimod (APD334) is a specific and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor (IC50: 1.88 nM in CHO cells).
Amiselimod hydrochloride
T10305CAS 942398-84-7
Amiselimod hydrochloride is a sphingosine 1-phosphate receptor-1 (S1P1) modulator.
ASP-4058
T10385CAS 952565-91-2
ASP-4058 is a selective and oral bioactive agonist for S1P1 and S1P5. It ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety pr...
KD-3010
T11747CAS 934760-92-6
KD-3010 is a orally, potent active, and selective PPARδ agonist.
PF-543 Citrate
T12436CAS 1415562-83-2
PF-543 Citrate is an inhibitor of sphingosine-competitive SPHK1(IC50 of 2 nM ).
PF429242 dihydrochloride
T12437CAS 2248666-66-0
PF429242 dihydrochloride is a reversible and competitive inhibitor of S1P (IC50 of 175 nM).
SK1-IN-1
T12927CAS 1218816-71-7
SK1-IN-1 is a potent inhibitor of sphingosine kinase 1 (SPHK1)(IC50 of 58 nM).
CYM50308
T15032CAS 1345858-76-5
CYM50308 is a high affinity agonist of sphingosine-1-phosphate receptor 4 (S1P4-R) (EC50: 56 nM). CYM50308 has no activity at S1P1-R, S1P2-R and S1P3-R subtypes...
TY-52156
T17183CAS 934369-14-9
TY-52156 is an effective and selective S1P3 receptor antagonist (Ki: 110 nM).
VPC 23019
T17237CAS 449173-19-7
VPC 23019 is a competitive antagonist at the S1P1 and S1P3 receptors (pKi= 7.86 and 5.93, respectively). It is also an agonist at the S1P4 and S1P5 receptors (p...
CYM5442
T2026CAS 1094042-01-9
CYM5442 is an S1P agonist, targeting to Sphingosine.
SEW2871
T2171CAS 256414-75-2
Sphingosine-1-phosphate receptor 1 agonist SEW2871 prolongs heterotopic heart allograft survival in mice.
CYM 5520
T22703CAS 1449747-00-5
noncompetitive allosteric agonist of S1P2
Fingolimod hydrochloride HOT
T2539CAS 162359-56-0
Fingolimod, a novel immune modulator, is a sphingosine 1-phosphate (S1P) antagonist (IC50: 0.033 nM in K562 and NK cells).
Ponesimod
T3258CAS 854107-55-4
Ponesimod is an orally available sphingosine-1-phosphate receptor 1 (S1PR1, S1P1) agonist that acts as a functional antagonist, with potential immunomodulating ...
CYM 5541
T3961CAS 945128-26-7
CYM-5541 is a selective and allosteric S1P3 receptor agonist.
S1p-receptor-agonist-1
T4031CAS 1514888-56-2
An S1P receptor agonist.
MHP
T4658CAS 1104874-94-3
MHP is an activator of sphingosine kinase (SPHK1), and significantly stimulates CAMP mRNA and protein production in KC.
PF543
T6085CAS 1415562-82-1
PF-543, a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 and Ki of 2.0 nM and 3.6 nM.
Siponimod
T6403CAS 1230487-00-9
BAF312 (Siponimod), 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 specif...
SKI II
T6673CAS 312636-16-1
SKI II is a highly selective and non-ATP-competitive S1P receptor inhibitor (IC50: 0.5 μM) while exhibiting no inhibitory action on other kinases including PKC...
ABC294640
T6750CAS 915385-81-8
ABC294640 is an orally active and specific sphingosine kinase-2 (SphK2) inhibitor (IC50: 60 μM).
Ozanimod
T6923CAS 1306760-87-1
Ozanimod (RPC1063) is a specific oral S1P Receptor 1 modulator. Ozanimod has been used in trials studying the treatment of Crohn's Disease, Ulcerative Colitis, ...
GSK2018682
T7360CAS 1034688-30-6
GSK2018682 is an agonist of sphingosine-1-phosphate receptor  (s1p1) and (s1p5) agonist(pEC50s of 7.7 and 7.2,respectively).
Fingolimod
T7939CAS 162359-55-9
Fingolimod is an antagonist of sphingosine 1-phosphate (S1P) (IC50 of 0.033 nM in K562 and NK cells).
SKI V
T8461CAS 24418-86-8
SKI V is a potent and noncompetitive non-lipid sphingosine kinase (SPHK; SK) inhibitor (GST-hSK,IC50 : 2 μM), and is a PI3K inhibitor(hPI3k,IC50 : 6 μM), indu...
PF-543
T8840CAS 1706522-79-3
PF-543 inhibits SphK1 with a K(i) of 3.6 nM, is sphingosine-competitive and is more than 100-fold selective for SphK1 over the SphK2 isoform.
SKI-178
T9014CAS 1259484-97-3
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 intrins...
K145 hydrochloride
TQ0138CAS 1449240-68-9
K145 is a specific inhibitor of SphK2 (IC50: 4.30 μM), while no inhibition of SphK1 at concentrations up to 10 μM.
Phorbol 12-myristate 13-acetate
TQ0198CAS 16561-29-8
Phorbol 12-myristate 13-acetate (PMA) is a dual SphK and PKC activator.
Etrasimod
TQ0227CAS 1206123-37-6
Etrasimod (APD334) is a specific and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor (IC50: 1.88 nM in CHO cells).