AM966

SKU: orb1302994

Description

AM966 is a potent, selective, and orally bioavailable LPA1 receptor antagonist with an IC50 of 17 nM. It effectively inhibits LPA-induced intracellular calcium mobilization. This compound is a valuable research tool for investigating LPA1-mediated pathways in fibrosis, cancer, and neuropathic pain in both cellular and animal models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1228690-19-4
• MW: 490.93
• Purity: 99.79% (May vary between batches)
• Formula: C₂₇H₂₃ClN₂O₅
• SMILES: C[C@@H](OC(=O)Nc1c(C)noc1-c1ccc(cc1)-c1ccc(CC(O)=O)cc1)c1ccccc1Cl
• Target: LPL Receptor,LPA Receptor
• Solubility: DMSO:45 mg/mL (91.66 mM);10% DMSO+90% Corn Oil:2 mg/mL (4.07 mM)

Bioactivity

• Target IC50:
  LPA1:IC50=17 nM
• In Vivo:
  In a 3-day bleomycin model, AM966 (30 mg/kg, BID) reduces vascular leakage, inflammation and lung injury and inflammation.
• In Vitro:
  Pre-treatment with AM966 (100 nM) completely blocks ERK1/2 phosphorylation induced by either amitriptyline or mianserin. LPA-induced ERK1/2 activation is completely blocked by AM966 (100 nM), which selectively antagonizes LPA1 over LPA2-5, with an IC50 value of 3.8±0.4 nM. AM966 inhibits LPA1-mediated chemotaxis of human A2058 melanoma cells (IC50=138±43 nM), IMR-90 human lung fibroblasts (IC50=182±86 nM) and CHO mLPA1 cells (IC50=469±54 nM).
• Cell Research:
  AM966 (Chem Scene, Monmouth Junction, NJ, USA) is dissolved in DMSO and stored, and then diluted with appropriate media (DMSO 0.5%) before use.CHO-K1 cells are grown to 80% confluency in 12-well plates, serum-starved for 24 h and incubated in serum-free medium with AM966. After 21 h, [3H]thymidine (0.5 μCi/well) is added and the incubation is continued for 3 h. The medium is then removed, and the cells are placed on ice and washed twice with 1 mL of ice-cold PBS containing 5% trichloroacetic acid. Cells are solubilized and [3H]thymidine incorporation is determined by liquid scintillation counting. Assays are performed in triplicate.
• Animal Research:
  In fasted mice, received AM966 (10 mg/kg), which is prepared in water, by oral gavage.

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

AM966, AM-966, AM 966, Lysophospholipid Receptor, LPA1, LPA Receptor, LPL, LPL Receptor, LPLReceptor, LPAReceptor, inhibit, Inhibitor

Compound Identifiers

PubChem CID

46240292