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; demonstrates promising pharmacokinetic properties and impressive in vivo efficacy in mouse model of infection comparable with those of the current oral antileishmanial miltefosine; 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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