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AN15368

Chemical Structure : AN15368

CAS No.: 2152662-92-3

AN15368 (AN 15368)

Catalog No.: PC-49314Not For Human Use, Lab Use Only.

AN15368 (AN 15368) is a small molecule prodrug activated by parasite carboxypeptidases to yield a compound that targets the messenger RNA processing pathway in Trypanosoma cruzi (T. cruzi), exhibits potent in vitro activity against T. cruzi with IC50 of 5 nM.

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    Biological Activity

    AN15368 (AN 15368) is a small molecule prodrug activated by parasite carboxypeptidases to yield a compound that targets the messenger RNA processing pathway in Trypanosoma cruzi (T. cruzi), exhibits potent in vitro activity against T. cruzi with IC50 of 5 nM.
    AN15368 could be cleaved by T. cruzi serine carboxypeptidase (CBP; TcCLB.508671.20) to generate the active form AN14667 in wild-type T. cruzi epimastigotes and amastigotes but not in the TcCLB knockout (KO) line
    AN15368 selectively targets CPSF3-mediated mRNA maturation in intracellular amastigotes.
    AN15368 (5 mg/kg, oral) cures T. cruzi infection in C57BL/6J mice infection model.
    AN15368 is orally bioactive and exhibits no overt toxicity in a 60 day course of treatment in non-human primates (NHPs).

    Physicochemical Properties

    M.Wt 389.255
    Formula C20H28BNO6
    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

    (tetrahydro-2H-pyran-4-yl)methyl (1-hydroxy-7-methyl-1,3-dihydrobenzo[c][1,2]oxaborole-6-carbonyl)-L-valinate

    References

    1. Angel M Padilla, et al. Nat Microbiol. 2022 Sep 5. doi: 10.1038/s41564-022-01211-y.

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