| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
ALDH1 AChE
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| ln Vitro |
In a dose-dependent way, α-NETA (50-150 nM; 24 hours) decreases the viability of all cell lines [3]. Membrane blebbing and cytoplasmic leaking are linked to the cell death of epithelial ovarian cancer (EOC) caused by α-NETA (2.5–10.0 μg/mL; 24 hours) [3]. In EOC cells, treatment with α-NETA leads to an upregulation of proteins associated to pyroptosis [3]. The purified enzyme assay of aldehyde dehydrogenase 1 family member A1 (ALDH1A1; IC50 = 0.04 μM) and G9a histone lysine amino acid methyltransferase (IC50 = 0.50 μM) are the next enzymes that are potently inhibited by α-NETA. The other enzymes are CMKLR1 (IC50 = 0.375 μM: β-ARR2 recruitment; cell-based test) and. α-NETA specifically prevents CMKLR1 from binding to β-arrestin2 when Chemerin is present [2]. α-NETA exhibits naphthyl fluorescence characteristics, with maximum emission at 437 nm and maximum excitation at 255 and 297 nm [1].
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| ln Vivo |
For 20 days, α-NETA (ip; 0.125 mg/kg; once every other day) dramatically lowered tumor weight and volume[3]. A 30 day course of α-NETA (sc injection; 3 mg/kg or 10 mg/kg; daily) at a dose of 3 mg/kg caused an average of 9 days before clinical symptoms were totally suppressed at a dose of 10 mg/kg[2].
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| Cell Assay |
Cell Viability Assay[3]
Cell Types: Ho8910, Ho8910PM, A2780, and Iose80 cells Tested Tested Concentrations: 50, 100, 150 nM Incubation Duration: 24 hrs (hours) Experimental Results: diminished all cell lines viability in a dose-dependent manner. Apoptosis Analysis[3] Cell Types: Epithelial ovarian cancer (EOC) cell Tested Tested Concentrations: 2.5, 7.5, 10.0 µg/mL Incubation Duration: 24 hrs (hours) Experimental Results: Led to EOC cell death associated with membrane blistering and cytoplasm leakage. |
| Animal Protocol |
Animal/Disease Models: BALB/c nude mice with skov3 cells[3]
Doses: 0.125 mg/kg Route of Administration: IP; once every other day for 20 days Experimental Results: Dramatically diminished tumor volume and tumor weight. |
| References |
[1]. Sastry BV, et al. Relationships between chemical structure and inhibition of choline acetyltransferase by 2-(alpha-naphthoyl)ethyltrimethylammonium and related compounds. Pharmacol Res Commun. 1988 Sep;20(9):751-71.
[2]. Graham KL, et al. A novel CMKLR1 small molecule antagonist suppresses CNS autoimmune inflammatory disease. PLoS One. 2014 Dec 1;9(12):e112925. [3]. Qiao L, et al. α-NETA induces pyroptosis of epithelial ovarian cancer cells through the GSDMD/caspase-4 pathway. FASEB J. 2019 Nov;33(11):12760-12767. |
| Molecular Formula |
C16H20INO
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|---|---|
| Molecular Weight |
369.24
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| CAS # |
115066-04-1
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| SMILES |
C(C1=CC=CC2=CC=CC=C12)(=O)CC[N+](C)(C)C.[I-]
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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: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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: 83.33 mg/mL (225.68 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.63 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL 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: ≥ 2.08 mg/mL (5.63 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.63 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7083 mL | 13.5413 mL | 27.0827 mL | |
| 5 mM | 0.5417 mL | 2.7083 mL | 5.4165 mL | |
| 10 mM | 0.2708 mL | 1.3541 mL | 2.7083 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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