ARN14974
Based on 1 Customer Validation
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.
- Purity: 99.29%
- CAS No.: 1644158-57-5
- Formula: C24H21FN2O3
- Molecular Weight:404.43
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Metabolism/Protease Compound Library
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.079 μM
Compound: 2c
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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
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[PMID: 32176488] |
| HEK293 | IC50 |
79 nM
Compound: 3; ARN14974
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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
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[PMID: 26560855] |
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 (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.
Chemical Information
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CAS No. 1644158-57-5
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Appearance Solid
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Molecular Weight 404.43
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Formula C24H21FN2O3
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Color Off-white to pink
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SMILES
O=C(N1C(OC2=CC(C3=CC=C(F)C=C3)=CC=C12)=O)NCCCCC4=CC=CC=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (270 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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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