Orlistat (Tetrahydrolipstatin) 是一种不可逆的胰腺和胃脂肪酶 (lipases) 抑制剂。 Orlistat也是一种脂肪酸合成酶 (FASN) 抑制剂，口服用于肥胖症的长期研究。具有抗动脉粥样硬化作用。
| 生物活性 | Orlistat (Tetrahydrolipstatin) is a well-known irreversible inhibitor of pancreatic and gastriclipases. Orlistat is also an inhibitor offatty acid synthase(FASN), is used orally for long-term research of obesity[1]. Anti-atherosclerotic effect[2]. |
体外研究
(In Vitro) | Orlistat (40 μM; 2 days) does not affect MGMT levels in a human melanoma cell line, but downregulates the repair protein by 30-70% in human peripheral blood mononuclear cells, in two leukemia and two colon cancer cell lines. Orlistat does not alter noticeably MGMT mRNA expression[1].
Western Blot Analysis[1] | Cell Line: | The human melanoma cell line M10, Peripheral blood mononuclear cells , The human Jurkat CD4+ T cell leukemia cell line, the human promyelocytic leukemia cell line HL-60, the epithelial colon cancer HCT116 cells,non adherent mononuclear cells (NAMNC)[1] | | Concentration: | 2.5, 5, 10, 20, 40 μM for Jurkat cells; 20 and 40 μM for HCT116 cells; 40 μM for normal NAMNC, M10 melanoma, HL-60 promyelocytic leukemia, and HT-29 colon cancer cells | | Incubation Time: | 2 days for Jurkat cells; 2 or 4 days for HCT116 cells; 2 days for NAMNC, M10 melanoma, HL-60 promyelocytic leukemia, HT-29 colon cancer | | Result: | Reduced by >50% the MGMT level at the concentration of 40 μM for Jurkat cells, whereas little or no effect was found when lower concentrations were used.
Downregulation of MGMT expression is produced at 40 μM for HCT116 cells.
Provoked an ~50% reduction of MGMT level at 40 μM in normal NAMNC, and HL-60 promyelocytic leukemia, HT-29 colon cancer cells except for melanoma M10 cells that showed no downregulation of the protein. |
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体内研究
(In Vivo) | Orlistat (10 mg/kg/day) significantly improves lipid profile, increases antioxidant enzymes and expression of anti-inflammatory markers, and decreases the expression of the pro-inflammatory marker compared to the obese (OB) group[2].
| Animal Model: | Eighteen male rats of Sprague–Dawley strain aged between 8–10 weeks weighing 200-250 g[2] | | Dosage: | 10 mg/kg/day | | Administration: | Orally; six weeks | | Result: | Treatment persistently restored the increased body weight, which was significantly observed at the ninth week until the end of the experimental period. |
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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 : 100 mg/mL(201.72 mM;Need ultrasonic) H2O :< 0.1 mg/mL(insoluble) 配制储备液 | 1 mM | 2.0172 mL | 10.0861 mL | 20.1723 mL | | 5 mM | 0.4034 mL | 2.0172 mL | 4.0345 mL | | 10 mM | 0.2017 mL | 1.0086 mL | 2.0172 mL |
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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 (5.04 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.04 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 (5.04 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (5.04 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 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 (5.04 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.04 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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