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编 号:F762843
分子式:C21H24ClN5O2
分子量:413.9
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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生物活性:
FNDR-20123 is a safe, first-in-class, and orally active anti-malarial HDAC inhibitor with IC50s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123 exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC50=41 nM) and sexual blood stage (IC50=190 nM for male gametocytes). FNDR-20123 inhibits HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 (IC50=25/29/2/11/282 nM, respectively.) and inhibits Class III HDAC isoforms at nanomolar concentrations.

体内研究:
FNDR-20123 (10-50 mg/kg; p.o.; bw for 4 days) is also able to reduce parasitaemia significantly in a mouse model for P. falciparum infection.Animal Model:P. falciparum Pf3D70087/N9 in NODscidIL2Rγnull mice (engrafted with human erythrocytes)
Dosage:10 and 50 mg/kg
Administration:P.o.; bw for 4 days
Result:Resulted in a significant reduction in parasitaemia with 6.5% and 2.57% parasitaemia at 10 and 50 mg/kg, respectively.

体外研究:
FNDR-20123 is active against all resistant strains tested so far, which will be highly valuable in eliminating the rapidly evolving drug-resistant parasite.
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