Leucomethylene blue mesylate(Synonyms: TRx0237 mesylate Methylene blue leuco base mesylate)

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Leucomethylene blue mesylate;(Synonyms: TRx0237 mesylate; Methylene blue leuco base mesylate) 纯度: 98.75%

Leucomethylene blue (TRx0237) mesylate 是具有口服活性的二代 tau 蛋白聚集的抑制剂 (Ki 值为0.12 μM)，可用于阿尔兹海默症的研究。Leucomethylene blue mesylate 是 Methylene blue (亚甲基蓝)的一种还原形式, 亚甲基蓝是一种化学指示剂和生物染色剂。

Leucomethylene blue mesylateamp;;(Synonyms: TRx0237 mesylate; Methylene blue leuco base mesylate)

Leucomethylene blue mesylate Chemical Structure

CAS No. : 1236208-20-0

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg) ; Apply now ;
10;mM;*;1 mL in DMSO ￥660 In-stock
5 mg ￥600 In-stock
10 mg ￥780 In-stock
50 mg ￥2300 In-stock
100 mg ￥4200 In-stock
200 mg ; 询价 ;
500 mg ; 询价 ;

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Leucomethylene blue mesylate 相关产品

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生物活性

Leucomethylene blue (TRx0237) mesylate, an orally active second-generation tau protein aggregation inhibitor (Ki of 0.12 μM), could be used for the study of Alzheimer’s Disease. Leucomethylene blue mesylate is a common reduced form of Methylene Blue, Methylene Blue is a member of the thiazine class of dyes[1][2][3].

IC50 Target

Ki: 0.12 μM (tau)[3].
体外研究
(In Vitro)

Leucomethylene blue (100 nM, 48 h) mesylate not only decreases the tau and p-tau expression levels, but also reversed the promoting effects of Aβ25-35 on orexin A and adenosine A1R expression levels[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[2]

Cell Line: Human SH-SY5Y cell line.
Concentration: 100 nM.
Incubation Time: 48 h.
Result: Aβ25-35 and TRx 0237 co-treatment significantly reversed the promoting effects of Aβ25-35 on tau, p-tau, orexin A and adenosine A1R expression.

分子量

477.62

Formula

C18H27N3O6S3
CAS 号

1236208-20-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4deg;C, stored under nitrogen, away from moisture

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (stored under nitrogen, away from moisture)
溶解性数据
In Vitro:;

DMSO : 110 mg/mL (230.31 mM; Need ultrasonic)

H2O : 83.33 mg/mL (174.47 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0937 mL 10.4686 mL 20.9371 mL
5 mM 0.4187 mL 2.0937 mL 4.1874 mL
10 mM 0.2094 mL 1.0469 mL 2.0937 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 (stored under nitrogen, away from moisture)。-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: ≥ 7.5 mg/mL (15.70 mM); Clear solution

    此方案可获得 ≥ 7.5 mg/mL (15.70 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 75.0 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: ≥ 2.75 mg/mL (5.76 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (5.76 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 27.5 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
*以上所有助溶剂都可在 MCE 网站选购。
参考文献

  • [1]. Gaudette NF, et al. Determination of methylene blue and leucomethylene blue in male and female Fischer 344 rat urine andB6C3F1 mouse urine. J Anal Toxicol. 2005 Jan-Feb;29(1):28-33.

    [2]. Zhenhua Liu, et al. Amyloid β and tau are involved in sleep disorder in Alzheimer’s disease by orexin A and adenosine A(1) receptor. Int J Mol Med. 2019 Jan;43(1):435-442.

    [3]. Francesco Panza, et al. Tau aggregation inhibitors: the future of Alzheimer’s pharmacotherapy? Expert Opin Pharmacother. 2016;17(4):457-61.