EIDD-2749 (4-Fluorouridine) is an orally active RdRp inhibitor. EIDD-2749 effectively blocks the replication of RSV and SARS-CoV-2. EIDD-2749 also exhibits activity against HCV and lymphocytic choriomeningitis virus (LCMV). EIDD-2749 is a promising oral therapeutic candidate for COVID-19 and is also suitable for research on other RNA viruses.
性状
Solid
IC50 & Target[1][2]
RdRp, RSV,SARS-CoV-2, HCV, COVID-19, LCMV.
体外研究(In Vitro)
EIDD-2749 induces a delayed stalling of phosphodiester bond formation by RSV and SARS-CoV-2 RdRP.EIDD-2749 is rapidly anabolizes, metabolically stable, and potently antiviral in disease-relevant well-differentiated HAE cultures.EIDD-2749 shows a ≥17-fold increase in anti-RSV potency relative to that on HEp-2 cells; however, the low cytotoxicity levels remains unchanged (CC50 169 mM), resulting in a high SI (SI = EC50/CC50) of ≥1877.EIDD-2749 inhibits SARS-CoV-2 with an EC50 value of 0.2-0.6 M.EIDD-2749 has an EC50 of 1.86 μM in theVero E6 cell line, cytotoxicity with a CC50 of 380 μM, and stability in human plasma. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
EIDD-2749 (0.2, 1, 5 mg/kg; p.o.; single daily for 4 days) shows good orally efficacious in RSV infection mice model in a dose-dependent manner.
EIDD-2749 shows high efficacious to SARS-CoV-2 infection and is effective with a single daily dose versus molnupiravir administered twice daily in vivo. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Sourimant J, et al. 4-Fluorouridine is an oral antiviral that blocks respiratory syncytial virus and SARS-CoV-2 replication. Science. 2022 Jan 14;375(6577):161-167. [2]. Abas AH, et al. 4’-fluorouridine and its derivatives as potential COVID-19 oral drugs: a review [version 1; peer review: 1 approved with reservations, 1 not approved]. F1000Research 2022, 11:410.
溶解度数据
In Vitro: H2O : 62.5 mg/mL (238.38 mM; Need ultrasonic)DMSO : 25 mg/mL (95.35 mM; Need ultrasonic)配制储备液