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MedChemExpress - Model Carmofur - ...

MedChemExpress - Model Carmofur - 61422-45-5

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].

Carmofur

MCE China：Carmofur

Brand：MedChemExpress (MCE)

Cat. No.HY-B0182

CAS：61422-45-5

Synonyms：HCFU

Purity：99.91%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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).

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].

IC50 & Target：IC50: 29 nM (acid ceramidase)[1]. N-Acylethanolamine Acidase (NAAA)[3]. Cellular Effect Cell Line Type Value Description References

References：

[1]. Jin Z, et al. Structural basis for the inhibition of SARS-CoV-2 main protease by antineoplastic drug carmofur. Nat Struct Mol Biol. 2020 Jun;27(6):529-532. [Content Brief]

[2]. Realini N, Solorzano C, Pagliuca C, et al. Discovery of highly potent acid ceramidase inhibitors with in vitro tumor chemosensitizing activity[J]. Scientific reports, 2013, 3(1): 1035. [Content Brief]

[3]. Wu K, et al. A new use for an old drug: carmofur attenuates lipopolysaccharide (LPS)-induced acute lung injury via inhibition of FAAH and NAAA activities[J]. Frontiers in pharmacology, 2019, 10: 818. [Content Brief]

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
•   The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects；
•   Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
•   It has a professional experimental center and strict quality control and verification system；
•   Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
•   The biological activity of the products has been verified by the experiments of customers in various countries；
•   A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
•   Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
•   It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。