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编 号:F741513
分子式:C23H26N2O2
分子量:362.46
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10mM*1mL in DMSO
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5mg
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10mg
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25mg
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50mg
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生物活性:
CHIKV-IN-2 is a potent inhibitor against Chikungunya virus (CHIKV), with excellent cellular antiviral activity (EC90=270 nM) and improved liver microsomal stability. CHIKV-IN-2 shows inhibitory activity against a cellular target Dihydroorotate Dehydrogenase (DHODH), which interacts with various viruses and regulate their replication via depleting intracellular pyrimidine pools.

体内研究:
CHIKV-IN-2 (compound 8q) (80 mg/kg; i.p. twice a day for 3 days) significantly decreases infectious CHIKV dissemination to other tissues of mice.CHIKV-IN-2 (40 mg/kg; p.o., i.p., s.c.) exhibits moderate bioavailability (F=41%, 43%, 4%), terminal elimination half-life (t1/2=9.9, 18.5, 18.6 h) and Cmax (642, 858, 90 ng/mL) in mice.CHIKV-IN-2 (1 mg/kg; i.v.) exhibits terminal elimination half-life (t1/2= 2.02 h) and AUC (497 h?ng/mL) in mice.Animal Model:Female and male C57BL/6 mice
Dosage:80 mg/kg
Administration:I.p. twice a day for 3 days
Result:Failed to inhibit virus loads at the site of infection.Decreased virus dissemination to other tissues.
Animal Model:Male C57BL/6 mice were challenged with CHIKV in the right footpad
Dosage:1 mg/kg for i.v. and 40 mg/kg for p.o., i.p., s.c. (Pharmacokinetic Analysis)
Administration:I.v., p.o., i.p., s.c.
Result:I.v.: t1/2= 2.02 h; AUC=497 h?ng/mL.P.o.: F=41%; t1/2=9.9 h; Cmax=642 ng/mL.I.p.: F=43%; t1/2=18.5 h; Cmax=858 ng/mL.S.c.: F=4%; t1/2=18.6 h; Cmax=90 ng/mL.

体外研究:
CHIKV-IN-2 (compound 8q) is a potent pan-alphavirus inhibitor, with EC90s of 0.85-2.5 μM for CHIKV clinical isolates and attenuated vaccine strains.CHIKV-IN-2 is active against alphavirus VEEV (EC90=0.40 μM) as well as flaviviruses such as West Nile Virus (WNV, EC90=0.20 μM) and Dengue Virus Strain-2 (DENV-2, EC90=0.60 μM).
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