AM095
| CAS No. | 1228690-36-5 | Cat. No. | BCP09983 |
| Name | AM095 | ||
| Synonyms | AM-095; AM 095; | ||
| Formula | C27H24N2O5 | M. Wt | 456.49 |
| Description | AM095 is an LPA1 receptor antagonist with good oral exposure and antifibrotic activity in rodent models. In vitro, AM095 inhibited GTPγS binding to Chinese hamster ovary (CHO) cell membranes overexpressing recombinant human or mouse LPA1 with IC50 values of 0.98 and 0.73 μM, respectively, and exhibited no LPA1 agonism. In functional assays, AM095 inhibited LPA-driven chemotaxis of CHO cells overexpressing mouse LPA? (IC50= 778 nM) and human A2058 melanoma cells (IC50 = 233 nM). Another study showed that LPA/LPA1 pathway inhibition has the potential to be an effective new therapeutic strategy for systemic sclerosis (SSc), and that LPA1 is an attractive pharmacologic target in dermal fibrosis. | ||
| Pathways | GPCR/G Protein | ||
| Targets | S1P Receptor | ||
Structure
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