Carmofur (Synonyms: HCFU)

Name: Carmofur
Brand: MedChemExpress
SKU: HY-B0182
Rating: 5.0 (3 reviews)

Cat. No.: HY-B0182 Purity: 99.91%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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).

For research use only. We do not sell to patients.

Carmofur Chemical Structure

CAS No. : 61422-45-5

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 66	In-stock	Estimated Time of Arrival: December 31
Solid
100 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 84	In-stock	Estimated Time of Arrival: December 31
1 g	USD 134	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Carmofur:

Carmofur (Standard) Get quote

3 Publications Citing Use of MCE Carmofur

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

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

Cellular Effect

Cell Line	Type	Value	Description	References
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]

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.

Molecular Weight

257.26

Formula

C₁₁H₁₆FN₃O₃

CAS No.

61422-45-5

Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.95%

Select Batch:

Data Sheet (277 KB) SDS (643 KB)

COA (244 KB) HNMR (170 KB) LCMS (470 KB)

Handling Instructions (2659 KB)

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]

Complete Stock Solution Preparation Table

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 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Carmofur (Synonyms: HCFU)

Customer Review

Other Forms of Carmofur:

Carmofur Related Antibodies

3 Publications Citing Use of MCE Carmofur

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

Carmofur Related Antibodies

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Complete Stock Solution Preparation Table

Carmofur Related Classifications

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