AM095 free acid

SKU: orb1310008

Description

AM095 (free acid) is a potent and selective antagonist of the LPA1 receptor, demonstrating sub-micromolar IC50 values against both human and mouse recombinant proteins. This small molecule inhibitor is a valuable research tool for investigating LPA1-mediated pathways in fibrosis, neuropathic pain, and cancer metastasis, as evidenced by its use in both in vitro and in vivo experimental models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1228690-36-5
• MW: 456.49
• Purity: 99.90%
• Formula: C₂₇H₂₄N₂O₅
• SMILES: C[C@@H](OC(=O)Nc1c(C)noc1-c1ccc(cc1)-c1ccc(CC(O)=O)cc1)c1ccccc1
• Target: LPA Receptor,LPL Receptor
• Solubility: 10% DMSO+90% Corn Oil:2.5 mg/mL (5.48 mM);DMSO:67.3 mg/mL (147.43 mM)

Bioactivity

• Target IC50:
  LPA1 (mouse):0.73 μM |LPA1 (human):0.98 μM
• 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.
• 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).

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AM095, AM-095, AM095 free acid, AM-095 free acid, AM 095, human LPA1, Inhibitor, mouse LPA1, inhibit, LPA1, LPA Receptor, LPAReceptor, LPLReceptor, LPL, LPL Receptor, Lysophospholipid Receptor

Compound Identifiers

PubChem CID

46213949