AM095

SKU: orb1306786

Description

AM095 is a potent and selective antagonist of the lysophosphatidic acid receptor 1 (LPA1), demonstrating IC50 values of 0.98 µM for human and 0.73 µM for mouse recombinant receptors. This small molecule is a valuable research tool for investigating LPA1-mediated pathways in fibrosis, neuropathic pain, and cancer metastasis in both cellular and animal models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1345614-59-6
• MW: 478.47
• Purity: 99.62% (May vary between batches)
• Formula: C₂₇H₂₃N₂NaO₅
• SMILES: [Na+].C[C@@H](OC(=O)Nc1c(C)noc1-c1ccc(cc1)-c1ccc(CC([O-])=O)cc1)c1ccccc1
• Target: LPL Receptor,LPA Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.09 mM);DMSO:5.5 mg/mL (11.49 mM)

Bioactivity

• Target IC50:
  LPA1 (recombinant human):0.98 μM|LPA1 (mouse):0.73 μM
• In Vivo:
  AM095 exhibits high oral bioavailability and moderate half-life, demonstrating tolerability in both rats and dogs following oral and intravenous administration. In rats, an oral dose (10 mg/kg) of AM095 results in peak plasma concentrations (Cmax) of 41 μM at 2 hours, decreasing to 10 nM by 24 hours. Conversely, an intravenous dose (2 mg/kg) leads to a Cmax of 12 μM within 15 minutes, similarly diminishing to approximately 10 nM by 24 hours, with a half-life (t1/2) of 1.79 hours. In dogs, an oral administration of 5 mg/kg achieves a peak plasma concentration of 21 μM within 15 minutes, falling to 10 nM by 24 hours, whereas an intravenous dosage (2 mg/kg) yields a Cmax of 11 μM in 15 minutes, reducing to 15 nM by 8 hours, and a t1/2 of 1.5 hours.
• In Vitro:
  AM095 is a potent LPA1 receptor antagonist because it inhibits 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 inhibits LPA-driven chemotaxis of CHO cells overexpressing mouse LPA1 (IC50=778 nM) and human A2058 melanoma cells (IC50=233 nM). The IC50 of AM095 in the human LPA1 GTPγS binding assay is comparable with that of our previously published compound AM966 (IC50=0.98±0.17 μM) and the Debio-0719 compound (IC50=0.60±0.04 μM). AM095 inhibits the LPA-induced calcium flux of CHO cells stably transfected with human or mouse LPA1. The IC50 for AM095 antagonism of LPA-induced calcium flux of human or mouse LPA1-transfected CHO cells is 0.025 and 0.023 μM, respectively.

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

AM 095, AM095, AM-095, Inhibitor, LPAReceptor, LPL, LPL Receptor, LPLReceptor, LPA Receptor, LPA1, Lysophospholipid Receptor, inhibit

Compound Identifiers

PubChem CID

53303875