Chemical Structure : GSK3494245
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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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.
M.Wt | 410.453 | |
Formula | C21H23FN6O2 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
1. Wyllie S, et al. Proc Natl Acad Sci U S A. 2019 Apr 8. pii: 201820175.
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