2. Metabolic Enzyme/Protease
  3. Ceramidase
  4. ARN14974

ARN14974, a benzoxazolone carboxamide, is a potent and systemically active inhibitors of intracellular acid ceramidase (IC50=79 nM).

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

ARN14974 Chemical Structure

ARN14974 Chemical Structure

CAS No. : 1644158-57-5

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5 mg USD 110 In-stock
10 mg USD 170 In-stock
50 mg USD 590 In-stock
100 mg USD 930 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

ARN14974 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

ARN14974, a benzoxazolone carboxamide, is a potent and systemically active inhibitors of intracellular acid ceramidase (IC50=79 nM)[1].

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
0.079 μM
Compound: 2c
Inhibition of human acid ceramidase expressed in HEK293 cells preincubated for 30 mins followed by fluorogenic probe addition and measured after 3 hrs by fluorescence based assay
Inhibition of human acid ceramidase expressed in HEK293 cells preincubated for 30 mins followed by fluorogenic probe addition and measured after 3 hrs by fluorescence based assay
[PMID: 32176488]
HEK293 IC50
79 nM
Compound: 3; ARN14974
Inhibition of recombinant human acid ceramidase expressed in HEK293 cells using N-[(1S,2R)-2-hydroxy-1-(hydroxymethyl)-4-(2-oxochromen-7-yl)-oxybutyl]dodecanamide substrate preincubated for 10 mins
Inhibition of recombinant human acid ceramidase expressed in HEK293 cells using N-[(1S,2R)-2-hydroxy-1-(hydroxymethyl)-4-(2-oxochromen-7-yl)-oxybutyl]dodecanamide substrate preincubated for 10 mins
[PMID: 26560855]
In Vitro

ARN14974 (20 μM; 24 hours; SW403 and Raw 264.7 cells) inhibits acid ceramidase (AC) in a complex cellular environment, leading to the intended biochemical response, that is, increased ceramide and decreased sphingosine levels[1].

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

ARN14974 Related Antibodies
In Vivo

ARN14974 (10 mg/kg; i.p.; mice) causes a substantial reduction in AC activity in multiple organs, including brain, liver, heart, lungs, and kidney[1].
ARN14974 (10 mg/kg; i.p.) quickly enters the bloodstream after a single intraperitoneal administration in mice, reaching a maximal plasma concentration, Cmax, of 1767.9 ng/mL and displaying a half-life time of 458 min in circulation. ARN14974 (1 mg/kg; i.v.) shows a Cmax and a half-life time of 628 ng/mL and 72 min, respectively[1].

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

404.43

Formula

C24H21FN2O3
CAS No.
Appearance

Solid

Color

Off-white to pink

SMILES

O=C(N1C(OC2=CC(C3=CC=C(F)C=C3)=CC=C12)=O)NCCCCC4=CC=CC=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (123.63 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4726 mL 12.3631 mL 24.7262 mL
5 mM 0.4945 mL 2.4726 mL 4.9452 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 (protect from light). 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: 1 mg/mL (2.47 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 1 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 (10.0 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% Corn Oil

    Solubility: ≥ 1 mg/mL (2.47 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 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 (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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
References

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 (protect from light). 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 2.4726 mL 12.3631 mL 24.7262 mL 61.8154 mL
5 mM 0.4945 mL 2.4726 mL 4.9452 mL 12.3631 mL
10 mM 0.2473 mL 1.2363 mL 2.4726 mL 6.1815 mL
15 mM 0.1648 mL 0.8242 mL 1.6484 mL 4.1210 mL
20 mM 0.1236 mL 0.6182 mL 1.2363 mL 3.0908 mL
25 mM 0.0989 mL 0.4945 mL 0.9890 mL 2.4726 mL
30 mM 0.0824 mL 0.4121 mL 0.8242 mL 2.0605 mL
40 mM 0.0618 mL 0.3091 mL 0.6182 mL 1.5454 mL
50 mM 0.0495 mL 0.2473 mL 0.4945 mL 1.2363 mL
60 mM 0.0412 mL 0.2061 mL 0.4121 mL 1.0303 mL
80 mM 0.0309 mL 0.1545 mL 0.3091 mL 0.7727 mL
100 mM 0.0247 mL 0.1236 mL 0.2473 mL 0.6182 mL
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ARN14974 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.

Keywords:

ARN149741644158-57-5ARN 14974ARN-14974Ceramidasebenzoxazolonecarboxamidesphingosinedysfunctionalceramide-mediatedsignalingInhibitorinhibitorinhibit

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