Otenaproxesul (ATB-346) 是具有口服活性的、非甾体抗炎药(NSAID)，可抑制环氧合酶-1 和 2(COX-1，2)。Otenaproxesul 具有抗炎生物活性，可用于缓解疼痛的研究。
| 生物活性 | Otenaproxesul (ATB-346), an orally active non-steroidal anti-inflammatory drug (NSAID), inhibitscyclooxygenase-1 and 2 (COX-1 and 2). Otenaproxesul possesses antiinflammatory and antinociceptive activities[1][4]. |
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体外研究
(In Vitro) | Otenaproxesul (100 μM) inhibits human melanoma cell proliferation by inhibiting pro-survival pathways associated with NF-B and Akt activation[2].
Otenaproxesul (100 μM) induces apoptosis of human melanoma cells[2].
Otenaproxesul (100 M) causes inhibition of IkB degradation and of NF-kB nuclear translocation as demonstrated by a reduction in band intensity of the p65 subunit in A375 cells[2].
Cell Proliferation Assay[2] | Cell Line: | A375 cells. | | Concentration: | 100 μM. | | Incubation Time: | 24, 48 and 72 h. | | Result: | Caused an inhibition of cell proliferation by 38.2%, 63.2% and 66%, respectively (P< 0.001). |
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体内研究
(In Vivo) | Otenaproxesul exhibits anti-inflammatory properties similar to naproxen, but with substantially reduced gastrointestinal toxicity[1].
Otenaproxesul (orally, 43 μmol/kg) inhibits growth of melanoma tumors in vivo and reduce plasma levels of melanoma-associated chemokines[2].
Otenaproxesul (orally, 16 mg/kg) results in significant inhibition of bone defect and other histological characteristics (such as flatness of the gingival epithelium, chronic inflammatory cell infiltration and loss of connective tissue in the gingival papillae). Otenaproxesul inhibits the increase of gingival IL-1β and IL-6 secondary to periodontitis, but IL-10 is unaffected[3].
| Animal Model: | Male, Wistar rats (200-225 g)[1]. | | Dosage: | 30, 60, 120 and 2740 μmol/kg. | | Administration: | Orally once. | | Result: | Inhibited PGE2 levels.
Suppressed TXB2 synthesis.
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| Animal Model: | Male, Wistar rats (200-225 g)[1]. | | Dosage: | 4 μmol/kg. | | Administration: | Orally twice daily, on days 7 to 21.
| | Result: | Significantly reduced 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 51.6 mg/mL(141.20 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 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 |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (6.84 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.84 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 *以上所有助溶剂都可在本网站选购。
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