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AM966 is a potent, selective, orally bioavailable LPA1 receptor antagonist. In vitro, AM966 inhibited LPA-stimulated intracellular calcium release (IC(50)= 17 nM) from Chinese hamster ovary cells stably expressing human LPA(1) receptors and inhibited LPA-induced chemotaxis (IC(50)= 181 nM) of human IMR-90 lung fibroblasts expressing LPA(1) receptors. AM966 (100 nM) completely blocked LPA-induced ERK1/2 activation, which selectively antagonizes LPA1 over LPA2-5, with an IC50 value of 3.8±0.4 nM. AM966 demonstrated a good pharmacokinetic profile following oral dosing in mice.
| Molecular Weight | 490.93 |
| Formula | C27H23ClN2O5 |
| CAS Number | 1228690-19-4 |
| Solubility (25°C) | DMSO: ≥ 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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