MSI-1436 lactate Trodusquemine lactate; Aminosterol-1436 lactate,99.67%

产品编号:Bellancom-12219A| CAS NO:1309370-86-2| 分子式:C40H78N4O8S| 分子量:1000.17

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货号 包装 价格 库存与货期 购买量 操作
Bellancom-12219A
5000.00 杭州 北京(现货)
Bellancom-12219A
9500.00 杭州 北京(现货)
Bellancom-12219A
16000.00 杭州 北京(现货)

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MSI-1436 lactate Trodusquemine lactate; Aminosterol-1436 lactate

产品介绍 MSI-1436 lactate 是具有选择性的 PTP1B 的非竞争性抑制剂,其 IC50 值为 1 μM,而对 TCPTP 的 IC50 值为 224 μM。
生物活性

MSI-1436 lactate is a selective, non-competitive inhibitor of the enzyme protein-tyrosine phosphatase 1B (PTP1B), with an IC50 of 1 μM, 200-fold preference over TCPTP (IC50 of 224 μM).

体外研究

MSI-1436's inhibition of TCPTP is approximately two logs less than the effect on PTP1B activity, with a resulting IC50 value of 224 µM. MSI-1436 (Trodusquemine, 10 μM) restores ERK phosphorylation in response to mGluR1/5 agonist DHPG in F11 neuronal cells. MSI-1436 (10 uM) rescues DHPG-induced holding currents and restores DSI in LMO4KO BLA neurons. MSI-1436 (0.1-100 µM) blocks PTP1B activity.

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

体内研究

MSI-1436 (10 mg/kg, i.p.) causes obesity-dependent body weight, reduces total body fat content and adipocyte size and lipid content of white adipose tissue of mice. MSI-1436 (Trodusquemine) exhibits anxiolytic effect through a restoration of endocannabinoid (eCB) signaling within the amygdala. MSI-1436 (5 mg/kg, i.p.) has an anti-diabetic effect on diabetic mice, and is sufficient to suppress food intake and cause weight loss in CD1 mice.

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

体内研究

MSI-1436 (10 mg/kg, i.p.) causes obesity-dependent body weight, reduces total body fat content and adipocyte size and lipid content of white adipose tissue of mice. MSI-1436 (Trodusquemine) exhibits anxiolytic effect through a restoration of endocannabinoid (eCB) signaling within the amygdala. MSI-1436 (5 mg/kg, i.p.) has an anti-diabetic effect on diabetic mice, and is sufficient to suppress food intake and cause weight loss in CD1 mice.

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

性状Solid
溶解性数据
In Vitro: 

DMSO : 54 mg/mL (53.99 mM; Need ultrasonic and warming)

0.1 M HCL : 50 mg/mL (49.99 mM; ultrasonic and adjust pH to 4 with HCl)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.9998 mL 4.9992 mL 9.9983 mL
5 mM 0.2000 mL 0.9998 mL 1.9997 mL
10 mM 0.1000 mL 0.4999 mL 0.9998 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 (sealed storage, 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: 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 3 mg/mL (3.00 mM); Clear solution

*以上所有助溶剂都可在 西域 网站选购。
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献

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