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GSK3494245

Chemical Structure : GSK3494245

CAS No.: 2080410-41-7

GSK3494245 (DDD01305143, GSK-3494245)

Catalog No.: PC-36167Not For Human Use, Lab Use Only.

GSK3494245 (DDD01305143, GSK-3494245) is a a preclinical candidate for Visceral leishmaniasis (VL) by inhibition of the chymotrypsin-like activity catalyzed by the β5 subunit of the L. donovani proteasome with IC50 of 0.16 uM.

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    Biological Activity

    GSK3494245 (DDD01305143, GSK-3494245) is a a preclinical candidate for Visceral leishmaniasis (VL) by inhibition of the chymotrypsin-like activity catalyzed by the β5 subunit of the L. donovani proteasome with IC50 of 0.16 uM.
    GSK3494245 demonstrates promising pharmacokinetic properties and impressive in vivo efficacy in mouse model of infection comparable with those of the current oral antileishmanial miltefosine.
    GSK3494245 shows potency against nonpathogenic Leishmania spp. Leishmania tarentolae (EC50=40 nM), which is comparable with that achieved against L. donovani promastigotes (EC50=14 nM); orally active.

    Physicochemical Properties

    M.Wt 410.453
    Formula C21H23FN6O2
    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

    N-(4-fluoro-3-(3-morpholinoimidazo[1,2-a]pyrimidin-7-yl)phenyl)pyrrolidine-1-carboxamide

    References

    1. Wyllie S, et al. Proc Natl Acad Sci U S A. 2019 Apr 8. pii: 201820175.

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