Carmofur (Synonyms: HCFU) |
Catalog No.GC12748
One-Click Copy Product Info
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Carmofur is a potent inhibitor of rat recombinant acid ceramidase with an IC50 value of 29nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 61422-45-5
Sample solution is provided at 25 µL, 10mM.
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Carmofur is a potent inhibitor of rat recombinant acid ceramidase with an IC50 value of 29nM [1]. Carmofur binds to the main protease (Mpro) of SARS-CoV-2, where the carbonyl group is covalently bound to catalytic Cys145 thus inhibiting the activity of Mpro[2]. Carmofur has been widely used to inhibit tumor progression and to block multidrug-resistant Streptococcus pneumoniae infection[3].
In vitro, Carmofur treatment for 24 hours significantly inhibited the proliferation of SJGBM2, CHLA200, and CHLA266 cells with IC50 values of 50µM, 13µM and 15µM, respectively[4]. Carmofur treatment for 12h significantly induced cell death in irradiated U87-10gy cells, accompanied by an increase in ceramide levels[5]. Treatment of U251T cells with 20µM Carmofur for 48 hours significantly promoted cell cycle alterations, induced apoptosis and decreased E2F8 mRNA expression in U251T cells [6].
In vivo, Carmofur treatment via oral administration at a dose of 10mg/kg (twice a day) for 3 days ameliorated the inflammatory responses and promoted the resolution of pulmonary injury in lipopolysaccharide (LPS)-treated mice[7]. Daily intraperitoneal injection of 750µg (dissolved in 100µl corn oil) of Carmofur for 10 days attenuated parasitemia and decreased reticulocyte frequency in mice during Plasmodium yoelii infection [8].
References:
[1] 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.
[2] Islam M M, Mirza S P. Versatile use of Carmofur: A comprehensive review of its chemistry and pharmacology[J]. Drug Development Research, 2022, 83(7): 1505-1518.
[3] Lyu W, Zhang Y, Zhang Z, et al. Carmofur Exhibits Antimicrobial Activity Against Streptococcus pneumoniae[J]. Antibiotics, 2025, 14(3): 231.
[4] Doan N B, Nguyen H S, Montoure A, et al. Acid ceramidase is a novel drug target for pediatric brain tumors[J]. Oncotarget, 2017, 8(15): 24753.
[5] Doan N B, Nguyen H S, Al-Gizawiy M M, et al. Acid ceramidase confers radioresistance to glioblastoma cells[J]. Oncology Reports, 2017, 38(4): 1932-1940.
[6] Hawkins C C, Jones A B, Gordon E R, et al. Carmofur prevents cell cycle progression by reducing E2F8 transcription in temozolomide-resistant glioblastoma cells[J]. Cell death discovery, 2023, 9(1): 451.
[7] Wu K, Xiu Y, Zhou P, 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.
[8] Günther A, Hose M, Abberger H, et al. The acid ceramidase/ceramide axis controls parasitemia in Plasmodium yoelii-infected mice by regulating erythropoiesis[J]. Elife, 2022, 11: e77975.
| Cell experiment [1]: | |
Cell lines | CHLA259 cells |
Preparation Method | CHLA259 cells were cultured in Iscove's modified Dulbecco's medium containing 20% fetal bovine serum (FBS), 4mM L-glutamine, 5μg/ml insulin, 5μg/ml transferrin, and 5ng/ml selenous acid at 37℃ in the presence of 5% CO2. Cells were plated onto a 96-well plate at a density of 1×105 cells/ml for 24h, and were treated with different concentrations of Carmofur (1, 10, 20, 40, 60, 80, and 100µM). After 24 hours, cell viability was analyzed. |
Reaction Conditions | 1, 10, 20, 40, 60, 80, and 100µM; 24h |
Applications | Carmofur treatment significantly decreased the cell viability of CHLA259 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Male C57BL/6J mice |
Preparation Method | Male C57BL/6J mice (20-22g) were randomly grouped, with eight mice for each group. Mice were anesthetized with chloral hydrate and instilled intratracheally with LPS (5mg/kg). Carmofur (10mg/kg; dissolved in saline with 5% polyethylene glycol 400 and 5% Tween 80) or vehicle was orally administered twice a day starting from the day of LPS application. Mice were sacrificed 3 days after LPS instillation. Mouse lung tissues were collected for analysis. |
Dosage form | 10mg/kg; twice a day for 3 days; p.o. |
Applications | Carmofur treatment ameliorated the inflammatory responses and promoted the resolution of pulmonary injury in mice. |
References: | |
| Cas No. | 61422-45-5 | SDF | |
| Synonyms | HCFU | ||
| Chemical Name | 5-fluoro-N-hexyl-2,4-dioxopyrimidine-1-carboxamide | ||
| Canonical SMILES | CCCCCCNC(=O)N1C=C(C(=O)NC1=O)F | ||
| Formula | C11H16FN3O3 | M.Wt | 257.26 |
| Solubility | ≥ 12.2mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.8871 mL | 19.4356 mL | 38.8712 mL |
| 5 mM | 777.4 μL | 3.8871 mL | 7.7742 mL |
| 10 mM | 388.7 μL | 1.9436 mL | 3.8871 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 15 reference(s) in Google Scholar.)