| S3572 |
BMS-986020 |
BMS-986020 (AM152, AP-3152 free acid) is a potent and selective antagonist of lysophosphatidic acid receptor 1 (LPA1). BMS-986020 inhibits bile acid and phospholipid transporters with IC50 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). |
Selective |
|
| S3534 |
AM966 |
AM966 is a high affinity, selective, oral Lysophosphatidic acid receptor 1 (LPA1) antagonist, which can inhibit LPA-stimulated intracellular calcium release (IC50=17 nM, by Ca flux assay). |
Selective |
LPA1, IC50: 17 nM |
| S8345 |
ONO-7300243 |
ONO-7300243 is a novel, potent LPA1(Lysophosphatidic Acid Receptor) antagonist with an IC50 of 160 nM. |
Selective |
LPA1, IC50: 0.16 μM |
| S2906 |
Ki16198 |
Ki16198 is the methyl ester of Ki16425, which is a LPA antagonist and inhibits LPA1- and LPA3-induced inositol phosphate production with Ki of 0.34 μM and 0.93 μM, respectively, shows weaker inhibition for LPA2, no activity at LPA4, LPA5, LPA6. |
Pan |
LPA1, Ki: 0.34 μM |
| S1315 |
Ki16425 |
Ki16425 is a competitive, potent and reversible antagonist to LPA1, LPA2 and LPA3 with Ki of 0.34 μM, 6.5 μM and 0.93 μM in RH7777 cell lines, respectively, shows no activity at LPA4, LPA5, LPA6. |
Pan |
LPA1, Ki: 0.34 μM |
