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AM095 free acid is a potent LPA1 receptor antagonist. AM095 free acid 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.
AM095 has high oral bioavailability and a moderate half-life and is well tolerated at the doses tested in rats and dogs after oral and intravenous dosing. AM095 dose-dependently reduces LPA-stimulated histamine release.
| Molecular Weight | 456.49 |
| Formula | C27H24N2O5 |
| CAS Number | 1228690-36-5 |
| Solubility (25°C) | DMSO: ≥ 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related LPL Receptor Products |
|---|
| Ki16425
Ki16425 is a LPA receptor antagonist with Ki values of 0.34, 6.5 and 0.93 μM for the human LPA1, LPA2 and LPA3 receptors, respectively. |
| 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. |
| GSK-2018682
This compound belongs to the class of organic compounds known as n-alkylindoles. These are compounds containing an indole moiety that carries an alkyl chain at the 1-position. |
| H2L5186303
H2L5186303 is a potent and selective LPA2 receptor antagonist with an IC50 of 9 nM. |
| AM095 sodium
AM095 is a potent and selective, orally bioavailable antagonist of lysophosphatidic acid receptor1 (LPA1). |
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