ARN14974 (Synonyms: Acid Ceramidase Inhibitor 17a) |
| Catalog No.GC13263 |
acid ceramidase inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1644158-57-5
Sample solution is provided at 25 µL, 10mM.
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IC50: 79 nM
ARN14974 is an acid ceramidase inhibitor.
The ceramides, a family of bioactive lipid-derived messengers, are involved in the control of cellular senescence, inflammation, as well as apoptosis. Ceramide hydrolysis by acid ceramidase (AC) can stop the biological activity of these substances and influence survival and function of normal and neoplastic cells.
In vitro: In a previous study, human colon adenocarcinoma SW403 cells and mouse macrophage-like Raw 264.7 cells were incubated in the presence of ARN14974. Results showed that ARN14974 could inhibit cellular AC activity with an IC50 of 825 nm in SW403 and 400 nm in Raw 264.7 cells. Moreover, consistent with these results, incubation with ARN14974 led to an increase in the levels of ceramide and a corresponding decrease in the levels of sphingosine [1].
In vivo: Injection of ARN14974 in mice was able to cause a substantial reduction in AC activity in multiple organs, including heart, lungs, brain, liver, and kidney. Highest levels of baseline AC activity and AC inhibition were found in lung tissue. As expected, the authors found a significant increase in ceramide species. Moreover, the levels of ceramides with longer fatty acyl chains were not affected. Furthermore, ARN14974 appeared to be well tolerated at the dosage tested [1].
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] D. Pizzirani, A. Bach, N. Realini, et al. Benzoxazolone carboxamides: Potent and systemically active inhibitors of intracellular acid ceramidase. Angewandte Chemistry International Edition English 54(2), 485-489 (2014).
| Cas No. | 1644158-57-5 | SDF | |
| Synonyms | Acid Ceramidase Inhibitor 17a | ||
| Chemical Name | 6-(4-fluorophenyl)-2-oxo-N-(4-phenylbutyl)-3(2H)-benzoxazolecarboxamide | ||
| Canonical SMILES | FC(C=C1)=CC=C1C2=CC=C3C(OC(N3C(NCCCCC4=CC=CC=C4)=O)=O)=C2 | ||
| Formula | C24H21FN2O3 | M.Wt | 404.4 |
| Solubility | ≤2mg/ml in DMSO;2mg/ml in dimethyl formamide | 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4728 mL | 12.364 mL | 24.728 mL |
| 5 mM | 0.4946 mL | 2.4728 mL | 4.9456 mL |
| 10 mM | 0.2473 mL | 1.2364 mL | 2.4728 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 ddH2O, 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)
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