CHIKV-IN-2 基孔肯雅病毒的选择性抑制剂，具有强大的细胞抗病毒活性 (EC90=270 nM) 以及能够改善肝微粒体稳定性。它能够抑制细胞靶二氢乳清酸脱氢酶的活性。

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[1].

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)[1]. 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[1].

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[1]. CHIKV-IN-2 (80 mg/kg; i.p. twice a day for 3 days) significantly decreases infectious CHIKV dissemination to other tissues of mice[1]. 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[1].

2361289-44-1

C23H26N2O2

362.46

DMSO:99 mg/mL (273.13 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years