| Name | AM095 free acid |
| Description | 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. |
| In vitro | In vitro, AM095 was a potent LPA receptor antagonist because it inhibited GTPγS binding to Chinese hamster ovary (CHO) cell membranes overexpressing recombinant human or mouse LPA with IC values of 0.98 and 0.73 μM, respectively, and exhibited no LPA agonism. In functional assays, AM095 inhibited LPA-driven chemotaxis of CHO cells overexpressing mouse LPA (IC = 778 nM) and human A2058 melanoma cells (IC = 233 nM)[3]. |
| In vivo | In vivo, AM095: 1) had high oral bioavailability and a moderate half-life and was well tolerated at the doses tested in rats and dogs after oral and intravenous dosing, 2) dose-dependently reduced LPA-stimulated histamine release, 3) attenuated bleomycin-induced increases in collagen, protein, and inflammatory cell infiltration in bronchalveolar lavage fluid, and 4) decreased kidney fibrosis in a mouse unilateral ureteral obstruction model[3]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 250 mg/mL (547.66 mM), Sonication and heating are recommended.
10% DMSO+90% Corn Oil : 2.5 mg/mL (5.48 mM), Sonication is recommended.
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| Keywords | mouse LPA1 | Lysophospholipid Receptor | LPLReceptor | LPL Receptor | LPL | LPAReceptor | LPA1 | LPA Receptor | Inhibitor | inhibit | human LPA1 | AM-095 free acid | AM095 free acid | AM-095 | AM095 | AM 095 |
| Inhibitors Related | Fingolimod hydrochloride | LX-2931 | Tyloxapol | Sphingosine-1-phosphate | CYM50374 | ASP-4058 | CAY10444 | Ki16198 | Siponimod | CYM5181 | Poloxamer 407 | S1PR1 modulator 1 |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | ReFRAME Related Library | Multi-Target Compound Library | Inhibitor Library | NO PAINS Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Compound Library |
United States
