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TG11-77

Chemical Structure : TG11-77

CAS No.: 2550393-38-7

TG11-77 (TG11-77 HCl)

Catalog No.: PC-49574Not For Human Use, Lab Use Only.

TG11-77 is a potent, selective, brain-permeable and orally available antagonist of the prostaglandin E2 (PGE2) receptor subtype EP2 with KB value of 9.7 nM.

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    Biological Activity

    TG11-77 is a potent, selective, brain-permeable and orally available antagonist of the prostaglandin E2 (PGE2) receptor subtype EP2 with KB value of 9.7 nM.
    TG11-77 is selective for EP2 over DP1, EP4, and IP receptors (KBs=7,320, 5,300, and >10,000 nM, respectively).
    TG11-77 inhibits the expression of genes encoding COX-2, IL-1β, and IL-6 induced by LPS and the EP2 receptor agonist ONO-AE1-259-01 in mouse BV-2 microglia expressing human EP2 receptors.
    TG11-77 eliminates the profound cognitive deficit in Y-maze performance after SE and reduces delayed mortality and microgliosis, with a minimum effective i.p. dose (as free base) of 8.8 mg/kg.

    Physicochemical Properties

    M.Wt 436.944
    Formula C23H25ClN6O
    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

    2-((4,6-dimethylpyridin-2-yl)amino)-N-(2-(2-methyl-1H-indol-3-yl)ethyl)pyrimidine-5-carboxamide, monohydrochloride

    References

    1. Radhika Amaradhi, et al. J Med Chem. 2020 Feb 13;63(3):1032-1050.

    2. Nicholas H Varvel , et al. Neuropharmacology. 2022 Nov 30;224:109356.

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