Cat. No.: HY-B0182

Carmofur

(Synonyms: HCFU)

6 Cited Publications

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Based on 6 publication(s) in Google Scholar

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).

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Pureté: 99.90%
CAS No.: 61422-45-5
Formule: C₁₁H₁₆FN₃O₃
Masse moléculaire:257.26

Stockage:

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

Carmofur Chemical Structure

CAS No.: 61422-45-5

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (6)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

IC50: 29 nM (acid ceramidase)^[1].
N-Acylethanolamine Acidase (NAAA)^[3].

Voir tous les produits spécifiques à Isoform Glutathione Peroxidase :

GPX1
GPX4

Cellular Effect

Cell Line	Type	Value	Description	References
Calu-3	CC₅₀	>100 μM Compound: 4a	Cytotoxicity against human Calu-3 cells measured after 2 days by MTT assay Cytotoxicity against human Calu-3 cells measured after 2 days by MTT assay	[PMID: 37633203]
HEK293	IC₅₀	0.029 μM Compound: 4a	Inhibition of rat recombinant acid ceramidase expressed in human HEK293 cells using N-lauroylceramide as substrate incubated for 30 mins prior to substrate addition measured after 30 mins by LC/MS analysis Inhibition of rat recombinant acid ceramidase expressed in human HEK293 cells using N-lauroylceramide as substrate incubated for 30 mins prior to substrate addition measured after 30 mins by LC/MS analysis	[PMID: 23614460]
HEK293	IC₅₀	20.7 nM Compound: Carmofur	Inhibition of human C-terminal His-tagged acid ceramidase variant 1 expressed in HEK293 cells using fluorogenic substrate Rbm-14-12 preincubated for 30 mins followed by substrate addition measured after 1 hr by fluorogenic assay Inhibition of human C-terminal His-tagged acid ceramidase variant 1 expressed in HEK293 cells using fluorogenic substrate Rbm-14-12 preincubated for 30 mins followed by substrate addition measured after 1 hr by fluorogenic assay	[PMID: 28603987]
Vero C1008	IC₅₀	0.67 μM Compound: 11	Antiviral activity against SARS-CoV-2 infected in African green monkey Vero E6 cells assessed as reduction in cell growth Antiviral activity against SARS-CoV-2 infected in African green monkey Vero E6 cells assessed as reduction in cell growth	[PMID: 37244162]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Real Time qPCR^[3]

Cell Line:

Raw264.7
Concentration:

10 μM. After LPS treatment (500 ng/mL; 72 h)
Incubation Time:

30 min
Result:

Effectively reduced the mRNA expression of pro-inflammatory cytokines such as IL-1β, IL-6, iNOS, TNF-α.

Western Blot Analysis^[3]

Cell Line:

Raw264.7
Concentration:

1 μM, 3 μM, 10 μM. After LPS treatment (500 ng/mL; 72 h)
Incubation Time:

30 min
Result:

Down-regulated the expression levels of p-p65 and p-κbα proteins in a dose-dependent manner, blocking the nuclear translocation of p65.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male C57BL/6J mice model of LPS-induced ALI^[3]
Dosage:

3 mg/kg, 10 mg/kg
Administration:

Oral gavage (p.o.), single dose. After LPS treatment (5 mg/kg; Tracheal perfusion, single dose)
Result:

Significantly inhibited MPO activity, which is a marker of neutrophil abundance.
Alleviated alveolar edema and inhibited neutrophil accumulation.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 61422-45-5
Appearance Solid
Masse moléculaire 257.26
Formule C₁₁H₁₆FN₃O₃
Color White to off-white
SMILES

O=C(N(C(N1)=O)C=C(F)C1=O)NCCCCCC
Synonyms

HCFU
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Publications (6)

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Journal Impact Factor

Signal Transduct Target Ther

Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]

2025 Dec 15;10(1):406. PMID: 41392286
Nucleic Acids Res

COVID19 Drug Repository: text-mining the literature in search of putative COVID19 therapeutics. [Abstract]

2021 Jan 8;49(D1):D1113-D1121. PMID: 33166390
ACS Cent Sci

Evaluation of SARS-CoV-2 Main Protease Inhibitors Using a Novel Cell-Based Assay. [Abstract]

2022 Feb 23;8(2):192-204. PMID: 35229034
J Mol Med (Berl)

Combination of PARP inhibitor and temozolomide to suppress chordoma progression. [Abstract]

2019 Aug;97(8):1183-1193. PMID: 31201471
Sci Rep

Cysteine-reactive mitigators of small vessel disease-related NOTCH3 mutants. [Abstract]

2026 Mar 20;16(1):14300. PMID: 41862552
bioRxiv

2025 Nov 17.

Solvant et solubilité

In Vitro:

DMSO : 83.33 mg/mL (323.91 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.8871 mL

19.4356 mL

38.8712 mL

5 mM

0.7774 mL

3.8871 mL

7.7742 mL

10 mM

0.3887 mL

1.9436 mL

3.8871 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.08 mg/mL (8.09 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (8.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (8.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 4

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 2 mg/mL (7.77 mM); Clear solution

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (277 KB)
SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Korean - KR (644 KB)
- Portuguese - PT (644 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.8871 mL	19.4356 mL	38.8712 mL	97.1779 mL
	5 mM	0.7774 mL	3.8871 mL	7.7742 mL	19.4356 mL
	10 mM	0.3887 mL	1.9436 mL	3.8871 mL	9.7178 mL
	15 mM	0.2591 mL	1.2957 mL	2.5914 mL	6.4785 mL
	20 mM	0.1944 mL	0.9718 mL	1.9436 mL	4.8589 mL
	25 mM	0.1555 mL	0.7774 mL	1.5548 mL	3.8871 mL
	30 mM	0.1296 mL	0.6479 mL	1.2957 mL	3.2393 mL
	40 mM	0.0972 mL	0.4859 mL	0.9718 mL	2.4294 mL
	50 mM	0.0777 mL	0.3887 mL	0.7774 mL	1.9436 mL
	60 mM	0.0648 mL	0.3239 mL	0.6479 mL	1.6196 mL
	80 mM	0.0486 mL	0.2429 mL	0.4859 mL	1.2147 mL
	100 mM	0.0389 mL	0.1944 mL	0.3887 mL	0.9718 mL

Carmofur

6 Cited Publications

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Carmofur

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Publications Citing Use of MedChemExpress (MCE) Carmofur

Voir tous les produits spécifiques à Isoform Glutathione Peroxidase

Activité biologique

Chemical Information

Publications (6)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Carmofur Related Classifications

HY-B0182 Related Classifications