Name: BQ-788 sodium salt
Price: 582.00 USD

- Overview
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    Background
    
    BQ-788 is a potent and selective antagonist of endothelin (ET) B-receptor with IC50 value of 1.2nM [1].
    In the in vitro assay, BQ-788 prevents ET-1 from binding to ETB receptors in human Girardi heart cells with IC50 value of 1.2nM. The inhibition to ETA receptors is much weaker with IC50 value of 1300nM. BQ-788 also inhibits ET binding to ETB receptors with IC50 values of 0.9nM and 1.2nM in porcine cerebellar membranes and hGH cells, respectively. The inhibition effects are quite poor in pCASM cells and SK-N-MC cells with IC50 values of 280nM and 1300nM, respectively. BQ-788 is specific to ET receptors. It cannot significantly inhibit other peptide hormone receptors at concentration of 10μM. It is found that BQ-788 interacts with ETB receptors competitively in hGH cells. Moreover, the in vivo assay demonstrates that ETB receptors are responsible for ET-1-elicited bronchoconstriction in guinea pigs [1].
    
    [1] Ishikawa K, Ihara M, Noguchi K, et al. Biochemical and pharmacological profile of a potent and selective endothelin B-receptor antagonist, BQ-788. Proceedings of the National Academy of Sciences, 1994, 91(11): 4892-4896.
- Properties
  - Categories
    
    ET B-receptor antagonist, potent and selective
    
    Alternative Name
    
    sodium;(2R)-2-[[(2R)-2-amino-3-(1-methoxycarbonylindol-3-yl)propanoyl]-[(2S)-2-[[(2R,6S)-2,6-dimethylpiperidine-1-carbonyl]amino]-4,4-dimethylpentanoyl]amino]hexanoate
    
    CAS Number
    
    156161-89-6
    
    Molecular Formula
    
    C34H50N5NaO7
    
    Molecular Weight
    
    663.78
    
    Appearance
    
    A solid
    
    Purity
    
    98.20%
    
    Solubility
    
    ≥33.2 mg/mL in DMSO; <2.69 mg/mL in H2O insoluble in; ≥2.79 mg/mL in EtOH
    
    Storage
    
    Desiccate at RT
    
    SMILES
    
    CCCCC(C(=O)[O-])N(C(=O)C(CC1=CN(C2=CC=CC=C21)C(=O)OC)N)C(=O)C(CC(C)(C)C)NC(=O)N3C(CCCC3C)C.[Na+]
    
    * For Research Use Only
- Reference
  - 1. Juliano T. Freitas, Jesus Lopez, et al. "The immunosuppressive role of Edn3 over‐expression in the melanoma microenvironment." Pigment Cell Melanoma Res. 2021 Nov;34(6):1084-1093. PMID:34288510
    2. Huang X, Chen C, et al. "Transdermal BQ-788/[email protected] quantum dots as targeting and smart tyrosinase inhibitors in melanocytes." Mater Sci Eng C Mater Biol Appl. 2019 Sep;102:45-52. PMID:31147016