Name: AM966
Price: 369.00 USD

- Overview
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    Background
    
    AM966 is a selective, potent and orally bioavailable antagonist of lysophosphatidic acid type 1 receptor (LPA1) with IC50 values of 17 and 19 nM for human or mouse LPA1, respectively [1]. Relative to LPA2, 3, 4, 5 receptors, AM966 shows 10-fold and 100-fold more selective in mouse and human cell lines for LPA1, respectively [1].
    In vitro, AM966 shows to inhibit LPA-induced chemotaxis in IMR-90 human lung fibroblasts, A2058 human melanoma cells and CHO cells expressing LPA1 receptors [1].
    In vivo, AM966 has been demonstrated to reduce total BALF cells, LDH activity, BALF collagen and total TGFβ concentrations in bleomycin-induced mice. Moreover, AM966 has been reported to block lung fibrosis, reduce lung inflammation and maintain body weight in mice induced by bleomycin [1].
- Properties
  - Categories
    
    LPA1 antagonist, oral active, high affinity, selective,
    
    Alternative Name
    
    AM 966;AM-966; 2-[4-[4-[4-[[(1R)-1-(2-chlorophenyl)ethoxy]carbonylamino]-3-methyl-1,2-oxazol-5-yl]phenyl]phenyl]acetic acid
    
    CAS Number
    
    1228690-19-4
    
    Molecular Formula
    
    C27H23ClN2O5
    
    Molecular Weight
    
    490.93
    
    Appearance
    
    A solid
    
    Purity
    
    99.36%
    
    Solubility
    
    ≥24.55 mg/mL in DMSO; insoluble in H2O; ≥2.24 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    CC1=NOC(=C1NC(=O)OC(C)C2=CC=CC=C2Cl)C3=CC=C(C=C3)C4=CC=C(C=C4)CC(=O)O
    
    * For Research Use Only
- Reference
  - 1. Li M, Lv Y, et al. "Co-stimulation of LPAR(1) and S1PR(1/3) increases the transplantation efficacy of human mesenchymal stem cells in drug-induced and alcoholic liver diseases." Stem Cell Res Ther. 2018 Jun 14;9(1):161. PMID:29898789
    2. Cai J, Wei J, et al."AM966, an Antagonist of Lysophosphatidic Acid Receptor 1, Increases Lung Microvascular Endothelial Permeability through Activation of Rho Signaling Pathway and Phosphorylation of VE-Cadherin. Mediators Inflamm."2017;2017:6893560. PMID:28348461