Oxiconazole (Ro 13-8996) nitrate 是一种广谱抗真菌剂,能抑制念珠菌 (Candida)、曲霉属真菌 (Aspergillus) 和毛癣菌属真菌 (Trichophyton) 的生长。Oxiconazole nitrate 也是一种高效的CYP3A4反式激活剂,可与利福平 (Rifampicin; HY-B0272) 竞争性拮抗。Oxiconazole nitrate 通过过氧化物酶 2 (PRDX2) 介导的细胞自噬 (autophagy) 停滞来发挥抑制结直肠癌的作用。
生物活性 | Oxiconazole (Ro 13-8996) nitrate is a broad spectrum anti-fungalagent which can inhibit the growth ofCandida,AspergillusandTrichophyton. Oxiconazole nitrate is also a highly efficacious activator ofCYP3A4transactivation, which could be antagonized byRifampicin(HY-B0272) in a competitive manner. Oxiconazole nitrate exhibits inhibitory effect against colorectalcancer(CRC) via peroxiredoxin-2 (PRDX2)-mediatedautophagyarrest[1][2][3]. |
IC50& Target[2] | |
体外研究 (In Vitro) | Oxiconazole (24 h; 0-40 μM) inhibits CRC cell growth[3]. Oxiconazole has antifungal activity againstCandida,AspergillusandTrichophyton[1]. Antifungal Activities of Oxiconazole[1].
| Candidaalbicans | Candidaglabrata | Candidaparapsilosis | Aspergillusfumigatus | Aspergillusflavus | Trichophytonmentagrophytes | Trichophytonrubrum | Oxiconazole | 0.03 μg/mL | 0.01 μg/mL | 0.008 μg/mL | 2 μg/mL | 2 μg/mL | 2 μg/mL | 2 μg/mL |
Cell Proliferation Assay[3] Cell Line: | HCT116, SW480, RKO, DLD-1, SW620, LoVo and NCM460 | Concentration: | 0-40 μM | Incubation Time: | 24 h | Result: | Exhibited inhibitory activity against HCT116, SW480, RKO, DLD-1, SW620, LoVo and NCM460 with IC50s of 25.86 μM, 27.34 μM, 21.01 μM, 25.56 μM, 21.75 μM, 24.87 μM and 126.4 μM. |
|
体内研究 (In Vivo) | Oxiconazole (50 mg/kg/day; IP; for 12 days) significantly restrains CRC cell growth[3].
Animal Model: | BALB/c nude mice (injected subcutaneously with HCT116 cells (1×107/mouse)[3] | Dosage: | 50 mg/kg/day | Administration: | IP; for 12 days | Result: | Significantly restrained CRC cell growth and showed no obvious side effects. |
|
Clinical Trial | |
分子量 | |
性状 | |
Formula | |
CAS 号 | |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(203.19 mM) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 2.0319 mL | 10.1597 mL | 20.3194 mL | 5 mM | 0.4064 mL | 2.0319 mL | 4.0639 mL | 10 mM | 0.2032 mL | 1.0160 mL | 2.0319 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 (sealed storage, away from moisture)。-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 (5.08 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.08 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。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (5.08 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.08 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 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (5.08 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.08 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
|