Carmofur

Carmofur (HCFU) is a rat recombinant acid ceramidase inhibitor with an IC₅₀ of 29 nM. Carmofur is also a protease inhibitor of SARS-CoV-2 main protease (Mpro), fatty acid amide hydrolase (FAAH) and N-acylethanolamine acid amidase (NAAA). Carmofur has anti-cancer, anti-inflammatory and anti-virus activities, and can be used for the study of COVID-19 and acute lung injury (ALI)^[1][2][3]. IC50 & Target:IC50: 29 nM (acid ceramidase)^[1].
N-Acylethanolamine Acidase (NAAA)^[3]. In Vitro:Carmofur (0.3-10 μM; 20 min-1 h) inhibits acid ceramidase (AC) activity in a concentration- and time-dependent manner in human colon cancer SW403 cells^[1].
Carmofur (1-100 μM) inhibits he activity of SARS-CoV-2 with an EC₅₀ of 24.3 μM in Vero E6 cells^[2].
Carmofur (5 μM; 6 h) inhibits the activities of FAAH and NAAH with IC₅₀ values of 0.11 μM and 0.71 μM, respectively, in HEK293 cells^[3].
Carmofur (10 μM; 30 min) has anti-inflammatory activity in Raw264.7 cells^[3]. In Vivo:Carmofur (10-30 mg/kg; Intraperitoneal injection (I.P.), single dose) inhibits acid ceramidase (AC) activity in various tissues, including lung and cerebral cortex, in male Swiss Webster mice^[1].
Carmofur (10 mg/kg; P.O. , single dose) significantly improves the LPS- (5 mg/kg; tracheal perfusion, single dose) (HY-D1056) induced inflammatory response by inhibiting the activities of FAAH and NAAA in in acute lung injury (ALI) mice, promoting the resolution of lung injury^[3].