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Purity: ≥98%
ATB-346, a structural analog of naproxen (one of the NSAIDs-Nonsteroidal anti-inflammatory drugs), is anti-inflammatory agent. ATB-346 was as effective as naproxen in adjuvant-induced arthritis in rats, with a more rapid onset of action. Unlike naproxen, ATB-346 did not increase blood pressure in hypertensive rats. Treatement with ATB-346 achieved a significantly more rapid and sustained recovery of motor function, obtaining greater than double the increase in locomotion score of the naproxen group by the 10th day of treatment. ATB-346 also significantly reduced the severity of inflammation (proinflammatory cytokines, apoptosis of neural tissue, and nitrosative stress) that characterized the secondary effects of SCI (spinal cord injury).
| ln Vitro |
At 100 μM, otenaproxesul suppresses the growth of human melanoma cells by blocking pro-survival pathways linked to Akt and NF-B activation[2]. Otenaproxesul (100 μM) causes human melanoma cells to undergo apoptosis[2]. Otenaproxesul (100 M) inhibits nuclear translocation of NF-kB and IkB degradation, as shown by a decrease in the p65 subunit's band intensity in A375 cells[2].
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| ln Vivo |
Similar to naproxen, otenaproxesul has anti-inflammatory qualities, but it is much less harmful to the gastrointestinal tract[1]. Melanoma tumor growth is inhibited in vivo by otenaproxesul (43 μmol/kg), which also lowers plasma levels of chemokines linked to melanoma[2]. (orally, 16 mg/kg) significantly inhibits bone defect and other histological features (including gingival epithelium flatness, chronic inflammatory cell infiltration, and gingival papillae connective tissue loss). Otenaproxesul does not alter IL-10 levels, but it does suppress the rise in gingival IL-1β and IL-6 brought on by periodontitis[3].
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| Cell Assay |
Cell Proliferation Assay[2]
Cell Types: A375 cells. Tested Concentrations: 100 μM. Incubation Duration: 24, 48 and 72 h. Experimental Results: Caused an inhibition of cell proliferation by 38.2%, 63.2% and 66%, respectively (P < 0.001). |
| Animal Protocol |
Animal/Disease Models: Male, Wistar rats (200-225 g)[1].
Doses: 30, 60, 120 and 2740 μmol/kg. Route of Administration: Orally once. Experimental Results: Inhibited PGE2 levels. Suppressed TXB2 synthesis. Animal/Disease Models: Male, Wistar rats (200-225 g)[1]. Doses: 4 μmol/kg. Route of Administration: Orally twice (two times) daily, on days 7 to 21 . Experimental Results: Dramatically decreased paw oedema at days 14 and 21 (*P < 0.05 vs. the vehicle-treated group). Caused markedly less gastric damage at all doses tested than naproxen. |
| References |
[1]. John L Wallace, et al. Markedly reduced toxicity of a hydrogen sulphide-releasing derivative of naproxen (ATB-346). Br J Pharmacol. 2010 Mar;159(6):1236-46.
[2]. Paola De Cicco, et al. ATB-346, a novel hydrogen sulfide-releasing anti-inflammatory drug, induces apoptosis of human melanoma cells and inhibits melanoma development in vivo. Pharmacol Res. 2016 Dec;114:67-73. [3]. Bruno Schneider Herrera, et al. The H2S-releasing naproxen derivative, ATB-346, inhibits alveolar bone loss and inflammation in rats with ligature-induced periodontitis. Med Gas Res. 2015 Feb 27;5:4. [4]. panelEduardoEkundi-Valentim, et al. P4 Antiinflammatory and antinociceptive effects of ATB-346, a gastric sparing hydrogen sulfide-releasing naproxen, in rats with carrageenan-induced knee joint synovitis. Nitric Oxide. Volume 27, Supplement 2, 15 September 2012, Page S13. |
| Molecular Formula |
C21H19NO3S
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| Molecular Weight |
365.45
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| CAS # |
1226895-20-0
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| Related CAS # |
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| SMILES |
CC(C1=CC=C2C=C(OC)C=CC2=C1)C(OC3=CC=C(C(N)=S)C=C3)=O
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.84 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 25.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7364 mL | 13.6818 mL | 27.3635 mL | |
| 5 mM | 0.5473 mL | 2.7364 mL | 5.4727 mL | |
| 10 mM | 0.2736 mL | 1.3682 mL | 2.7364 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.
 Effects of naproxen and two hydrogen sulphide-releasing naproxen derivatives (ATB-345 and ATB-346) in a model of zymosan-induced inflammation in the mouse.
ATB-346 spares the stomach of injury in circumstances in which gastric mucosal defence is impaired.Br J Pharmacol.2010 Mar;159(6):1236-46. |
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 ATB-346 protected the small intestine from damage and bleeding.
Oral administration of naproxen caused haemorrhagic damage in the stomach that increased in severity in a dose-dependent manner. In contrast, ATB-346 administration caused markedly less gastric damage at all doses tested.Br J Pharmacol.2010 Mar;159(6):1236-46. |
 Effects of naproxen, ATB-346 and celecoxib on healing of gastric ulcers in mice.
Unlike conventional NSAIDs (diclofenac and naproxen at 60 and 90 µmol·kg−1respectively), equimolar doses of hydrogen sulphide-releasing derivatives of these drugs (ATB-337 and ATB-346 respectively) did not significantly elevate mean arterial blood pressure in rats with hypertension induced by addition of L-NAME to the drinking water (400 mg·L−1).Br J Pharmacol.2010 Mar;159(6):1236-46. |
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