Pantoprazole sodium (BY1023 sodium) 是一种具有口服活性的,有效质子泵 (proton pump) 抑制剂 (PPI)。Pantoprazole sodium 是一种取代的苯并咪唑,是一种有效的H+/K+-ATPase抑制剂,IC50为 6.8 μM。Pantoprazo sodium 可以改善 pH 值稳定性,并具有抗分泌,抗溃疡的作用。Pantoprazo sodium 联合阿霉素 (Doxorubicin; HY-15142) 可显着增加肿瘤生长延迟。
生物活性 | Pantoprazole sodium (BY10232 sodium) is an orally active and potentproton pumpinhibitor (PPI)[1]. Pantoprazole sodium, a substituted benzimidazole, is a potentH+/K+-ATPaseinhibitor with anIC50of 6.8 μM. Pantoprazole sodium improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole sodium significantly increased tumor growth delay combined with Doxorubicin (HY-15142)[3][4]. |
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体外研究 (In Vitro) | Pantoprazole sodium (BY1023 sodium; 1-10000 μM) leads to concentration-dependent increases in endosomal pH in EMT-6 and MCF7 cells[1]. Pantoprazole sodium can block exosome release. Pantoprazole sodium inhibits the activity of V-H+-ATPase and impaires the ability of tumour cells (melanomas, adenocarcinomas, and lymphoma cell lines) to acidify the extracellular medium[2]
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体内研究 (In Vivo) | Pantoprazole sodium (BY1023 sodium; 200 mg/kg; IP; once a week for 3 weeks) significantly increases tumor growth delay of MCF-7 xenografts combined with Doxorubicin[1]. Pantoprazole sodium (0.3-3 mg/kg, p.o.) dose-dependently decreases both basal acid secretion in pylorus-ligated rats and the stimulated acid secretion induced by mepirizole in acute fistula rats[4].
Animal Model: | Mice bearing MCF-7 or A431 xenografts[1] | Dosage: | 200 mg/kg | Administration: | IP; once a week for 3 weeks; alone or 2 hours before Doxorubicin (6 mg/kg i.v.) | Result: | Showed even greater growth delay of MCF-7 xenografts with Doxorubicin compared with the single-dose combination. Significantly increased tumor growth delay with a single dose with Doxorubicin. There is no effect on growth delay alone.
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(246.70 mM) H2O : 3.85 mg/mL(9.50 mM;Need ultrasonic) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 2.4670 mL | 12.3350 mL | 24.6700 mL | 5 mM | 0.4934 mL | 2.4670 mL | 4.9340 mL | 10 mM | 0.2467 mL | 1.2335 mL | 2.4670 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 and light)。-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: PBS Solubility: 8.33 mg/mL (20.55 mM); Clear solution; Need ultrasonic and warming and heat to 60℃ 2. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (6.17 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.17 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。 3. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (6.17 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.17 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。 4. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (6.17 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.17 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。
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