Malotilate (NKK 105) 是一种口服活性的促肝药，是一种抗纤维化物质，可选择性抑制5-lipoxygenase (5-LOX)(IC50=4.7 μM)。 Malotilate 通过降低肝脏乙醛水平并防止转铁蛋白保留在肝细胞中，从而预防了酒精-吡唑肝炎中肝细胞损伤的发展。
| 生物活性 | Malotilate (NKK 105), an orally active hepatotropic agent and an anti-fibrotic substance, selectively inhibits the5-lipoxygenase (5-LOX)(IC50=4.7 μM). Malotilate prevents the development of hepatocytic injury in alcohol-pyrazole hepatitis by decreasing hepatic acetaldehyde levels and preventing the retention of transferrin in the hepatocytes[1][2]. |
| IC50& Target | 5-Lipoxygenase 4.7 μM (IC50) |
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体外研究
(In Vitro) | Malotilate reduces collagen synthesis and cell migration activity of fibroblasts in vitro[3].
Malotilate, an anti-fibrotic substance, selectively inhibited the 5-lipoxygenase, whereas both the 12- and the 15-lipoxygenase pathways are stimulated. Malotilate has been shown to prevent acute experimental liver injury induced by several hepatotoxic compounds, including Ahyl alcohot, Bromobenzene, Carbon tetrachloride, ChIoroform, Dimethylnitrosamine and Thioacetamide[4].
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体内研究
(In Vivo) | Malotilate (100 mg/kg; p.o.; daily for 3 days) treatment in rats with hypocholesterolemia results in a rapid normalization of lowered serum cholesterol[5].
| Animal Model: | Male rats of the SLC-SD strain (rats with carbon tetrachloride-induced liver damage)[5] | | Dosage: | 100 mg/kg | | Administration: | P.o.; daily for 3 days | | Result: | The triglyceride secretion from livers in rats given CCI4 was inhibited to about 40% of the level in the control rats. This inhibition of the triglyceride secretion was completely normalized in response to malotilate administration for 3 days. |
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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(346.76 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 3.4676 mL | 17.3382 mL | 34.6765 mL | | 5 mM | 0.6935 mL | 3.4676 mL | 6.9353 mL | | 10 mM | 0.3468 mL | 1.7338 mL | 3.4676 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 (8.67 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.67 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 (8.67 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.67 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 (8.67 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.67 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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