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TG8-260

Chemical Structure : TG8-260

CAS No.: 2490544-50-6

TG8-260 (TG 8-260)

Catalog No.: PC-72851Not For Human Use, Lab Use Only.

TG8-260 is a second-generation, potent, selective EP2 antagonist with Schild KB of 13.2 nM.

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    Biological Activity

    TG8-260 is a second-generation, potent, selective EP2 antagonist with Schild KB of 13.2 nM.
    TG8-260 displays 500-fold selectivity to EP2 against other prostanoid receptors.
    TG8-260 has a plasma half-life of 2.14 h (PO) and excellent oral bioavailability (77.3%), TG8-260 is a potent inhibitor of CYP450 enzymes.
    TG8-260 displays antagonistic activity on the induction of EP2 receptor-mediated inflammatory gene expression in microglia BV2-hEP2 cells.
    TG8-260 reduces hippocampal neuroinflammation and gliosis after pilocarpine-induced status epilepticus in rats.
    TG8-260 is a tool for investigating anti-inflammatory pathways in peripheral inflammatory disease animal models.

    Physicochemical Properties

    M.Wt 344.418
    Formula C21H20N4O
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    4-(1H-imidazol-4-yl)-N-(2-(2-methyl-1H-indol-3-yl)ethyl)benzamide

    References

    1. Radhika Amaradhi, et al. ACS Pharmacol Transl Sci. 2022 Jan 25;5(2):118-133.

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