CHIKV-IN-2

Research use only, not for human use.

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.

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. Therefore, CHIKV-IN-2 is a potent inhibitor against Chikungunya virus (CHIKV), with excellent cellular antiviral activity (EC90=270 nM) and improved liver microsomal stability.(In Vitro):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). CHIKV-IN-2 is a potent pan-alphavirus inhibitor, with EC90s of 0.85-2.5 μM for CHIKV clinical isolates and attenuated vaccine strains.(In Vivo):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 (80 mg/kg; i.p. twice a day for 3 days) significantly decreases infectious CHIKV dissemination to other tissues of 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.

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Metabolic Enzyme/Protease

Dehydrogenase

NAE

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2361289-44-1

362.5

C23H26N2O2

>98% (HPLC)

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CC(C)(c(cc1)ccc1NC(c(cc(CCCCC1)c1c1)c1OC)=O)C#N

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(-20℃)

With Ice Pack

≥ 2 years