| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
ARN14974 (ARN-14974), a benzoxazolone carboxamide analog, is a novel and potent inhibitor of acid ceramidase with IC50 of 79 nM. It inhibits acid ceramidase activity, reduces levels of sphingosine and dihydroceramide, and increases levels of ceramide in SW403 adenocarcinoma cells and RAW 264.7 murine macrophages when used at concentrations ranging from 0.1 to 20 mM. In vivo, ARN14974 (10 mg/kg, i.v.) reduces acid ceramidase activity in multiple organs, including brain, liver, heart, lungs, and kidney, and increases pulmonary ceramide levels in mice.
| ln Vitro |
In complicated cellular settings, ARN14974 (20 μM; 24 hours; SW403 and Raw 264.7 cells) inhibits acid ceramidase (AC), leading to the anticipated biochemical reactions of elevated ceramide and lowered sphingosine levels [1].
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| ln Vivo |
ARN14974 (10 mg/kg; i.p.; mice) significantly lowers the activity of AC in a number of organs, including the kidneys, liver, heart, brain, and lungs [1]. After a single intraperitoneal injection of 10 mg/kg, ARN14974 (10 mg/kg) enters the bloodstream quickly in mice, with a maximum plasma concentration Cmax of 1767.9 ng/mL and a circulating half-life of 458 minutes. The Cmax and half-life of ARN14974 (1 mg/kg; intravenous) are 628 ng/mL and 72 minutes, respectively [1].
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| References |
| Molecular Formula |
C24H21FN2O3
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|---|---|
| Molecular Weight |
404.433549642563
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| Exact Mass |
404.153
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| Elemental Analysis |
C, 71.27; H, 5.23; F, 4.70; N, 6.93; O, 11.87
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| CAS # |
1644158-57-5
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| PubChem CID |
101913546
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| Appearance |
Off-white to pink solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.613
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| LogP |
5.4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
30
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| Complexity |
587
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1C=CC(=CC=1)C1C=CC2=C(C=1)OC(N2C(NCCCCC1C=CC=CC=1)=O)=O
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| InChi Key |
DPYVAZSLMQCVOG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H21FN2O3/c25-20-12-9-18(10-13-20)19-11-14-21-22(16-19)30-24(29)27(21)23(28)26-15-5-4-8-17-6-2-1-3-7-17/h1-3,6-7,9-14,16H,4-5,8,15H2,(H,26,28)
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| Chemical Name |
6-(4-fluorophenyl)-2-oxo-N-(4-phenylbutyl)-3(2H)-benzoxazolecarboxamide
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| Synonyms |
ARN-14974; ARN14974; ARN 14974; Acid Ceramidase Inhibitor 17a;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~123.63 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 1 mg/mL (2.47 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1 mg/mL (2.47 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2473 mL | 1.2363 mL | 2.4726 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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