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GSK3494245

Chemical Structure : GSK3494245

CAS No.: 2080410-41-7

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GSK3494245 (DDD01305143, GSK-3494245)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    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.

    物理化学性质&存储条件

    分子量 410.453
    分子式 C21H23FN6O2
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20 °C 12 个月; 4°C 6 个月
    配置液
    -80 °C 6 个月; -20°C 6 个月
    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

    参考文献

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

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