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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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Purity & Documentation Purity: >98% (HPLC)

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; 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.

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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