lysophospholipid receptor

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.

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

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.

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

AM095 (free acid) is a potent LPA1 receptor antagonist with IC50 values of 0.98 μM for recombinant human LPA1 and 0.73 μM for recombinant mouse LPA1.

Amiselimod hydrochloride (MT-1303 hydrochloride) is a sphingosine 1-phosphate receptor-1 (S1P1) modulator.

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

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 at concentrations up to 25 μM and it shows 37-fold more selective for S1P4-R than S1P5-R.

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).

TY-52156 is an effective and selective S1P3 receptor antagonist (Ki: 110 nM).

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 (pEC50= 6.58 and 7.07, respectively).

AM095 is a potent LPA1 receptor antagonist with IC50 values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 respectively.

CYM5442 is an S1P agonist, targeting to Sphingosine.

ML-031 activated S1P2 with an EC50 value of 1 μM in an S1P reporter assay.

ML-178, a dichlorobenzene, is a potent and selective agonist of sphingosine-1-phosphate receptor 4 (S1PR4), with an EC50 of 46 nM, and has no effect on other S1P receptors at a concentration of 25 μM.

CS 2100 (1-[[4-Ethyl-5-[5-(4-phenoxyphenyl)-1,2,4-oxadiazol-3-yl]-2-thienyl]methyl]-3-azetidinecarboxylic acid) is an S1P1 agonist.

CYM-5520 is a noncompetitive allosteric agonist of S1P2

H2L 5765834 is a lysophosphatidic acid receptors antagonist

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.

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

CYM-5541 (ML249) is a selective and allosteric S1P3 receptor agonist.

BMS-986020 (AM152) is a selective LPA1 antagonist.

S1p receptor agonist 1 (S1p-receptor-agonist-1) is an S1P receptor agonist.

AM966, a excellent affinity, specific, oral LPA1(IC50=17 nM) antagonist, suppresses LPA-stimulated intracellular calcium release.