ARN14974

Alias: ARN-14974; ARN14974; ARN 14974; Acid Ceramidase Inhibitor 17a;
Cat No.:V3381 Purity: ≥98%
ARN14974 (ARN-14974), a benzoxazolone carboxamide analog, is a novel and potent inhibitor of acid ceramidase with IC50of 79 nM.
ARN14974 Chemical Structure CAS No.: 1644158-57-5
Product category: Ceramidase
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

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.

Biological Activity I Assay Protocols (From Reference)
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].
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].
References
[1]. Pizzirani D, et al. Benzoxazolone carboxamides: potent and systemically active inhibitors of intracellular acid ceramidase. Angew Chem Int Ed Engl. 2015;54(2):485-489.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C24H21FN2O3
Molecular Weight
404.433549642563
CAS #
1644158-57-5
SMILES
O=C(N1C(OC2=CC(C3=CC=C(F)C=C3)=CC=C12)=O)NCCCCC4=CC=CC=C4
InChi Key
DPYVAZSLMQCVOG-UHFFFAOYSA-N
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)
Chemical Name
6-(4-fluorophenyl)-2-oxo-N-(4-phenylbutyl)-3(2H)-benzoxazolecarboxamide
Synonyms
ARN-14974; ARN14974; ARN 14974; Acid Ceramidase Inhibitor 17a;
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~50 mg/mL (~123.63 mM)
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.

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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.
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