Malotilate(Synonyms: 马洛替酯; NKK 105)

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Malotilate (Synonyms: 马洛替酯; NKK 105) 纯度: 99.54%

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。

Malotilate(Synonyms: 马洛替酯; NKK 105)

Malotilate Chemical Structure

CAS No. : 59937-28-9

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10 mM * 1 mL in DMSO ￥768 In-stock
10 mg ￥698 In-stock
50 mg ￥1162 In-stock
100 mg ￥1953 In-stock
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生物活性

Malotilate (NKK 105), an orally active hepatotropic agent and an anti-fibrotic substance, selectively inhibits the 5-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)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

288.38

Formula

C12H16O4S2
CAS 号

59937-28-9
中文名称

马洛替酯；二噻茂醋
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
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (346.76 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 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 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Matsuda Y, et al. Effects of malotilate on alcoholic liver injury in rats. Alcohol Clin Exp Res. 1988;12(5):665-670.

    [2]. Vermeer MA, Wilson JH, Zijlstra FJ, Vincent JE. Differential effects of malotilate on 5-, 12- and 15-lipoxygenase in human ascites cells. Agents Actions. 1989;26(1-2):252-253.

    [3]. Poeschl A, et al. Malotilate reduces collagen synthesis and cell migration activity of fibroblasts in vitro. Biochem Pharmacol. 1987;36(22):3957-3963.

    [4]. Zijlstra FJ, et al. Differential effects of malotilate on 5-, 12- and 15-lipoxygenase in human ascites cells. Eur J Pharmacol. 1989;159(3):291-295.

    [5]. Wakasugi J, et al. Action of malotilate on reduced serum cholesterol level in rats with carbon tetrachloride-induced liver damage. Jpn J Pharmacol. 1985;38(4):391-401.

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