ARN14974
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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).
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 404.4 |
Cas No. | 1644158-57-5 |
Formula | C24H21FN2O3 |
Synonyms | Acid Ceramidase Inhibitor 17a |
Solubility | ≤2mg/ml in DMSO;2mg/ml in dimethyl formamide |
Chemical Name | 6-(4-fluorophenyl)-2-oxo-N-(4-phenylbutyl)-3(2H)-benzoxazolecarboxamide |
SDF | Download SDF |
Canonical SMILES | FC(C=C1)=CC=C1C2=CC=C3C(OC(N3C(NCCCCC4=CC=CC=C4)=O)=O)=C2 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |