SRT 2104

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SRT 2104  纯度: 99.76%

SRT 2104 是一种首创、高度选择性、可通过血脑屏障的 Sirt1 (依赖于 NAD+) 激活剂，增加 Sirt1 蛋白水平，但对其 mRNA 无作用。用于糖尿病和亨廷顿氏症的研究。

SRT 2104

SRT 2104 Chemical Structure

CAS No. : 1093403-33-8

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生物活性

SRT 2104 is a first-in-class, highly selective and brain-permeable activator of the NAD+ dependent deacetylase Sirt1, increases Sirt1 protein, but shows no effect on Sirt1 mRNA. Used in the research of diabetes mellitus and Huntington’s disease[1][2][3].

IC50 & Target

SIRT1

 

体内研究
(In Vivo)

SRT 2104 (100 mg/kg/day, supplemented in diet for 24 weeks) increases SIRT1 protein without altering Sirt1 mRNA in diabetic mice[2].
SRT 2104 (100 mg/kg/day, supplemented in diet for 24 weeks) decreases testicular oxidative stress, activation of apoptotic signaling, and ER stress in diabetic mice[2].
SRT 2104 (0.5%; for 18 weeks) improves motor function and increases survival in N171-82Q HD mice[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL/6 mice (8-week-old)[2]
Dosage: 100 mg/kg/day
Administration: Supplemented in diet for 24 weeks
Result: Enhanced SIRT1 protein without evelating Sirt1 mRNA level. Attenuated diabetes mellitus (DM)-induced oxidative stress, apoptotic signaling, and ER stress.
Animal Model: WT and N171-82Q HD mice (6 weeks old)[3]
Dosage: 0.5%
Administration: 0.5% SRT 2104 containing diet for 6, 12, 18 weeks
Result: Ameliorated motor deficits and increased survival in N171-82Q HD mice.

Clinical Trial

分子量

516.64

Formula

C26H24N6O2S2
CAS 号

1093403-33-8
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 : 5 mg/mL (9.68 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9356 mL 9.6779 mL 19.3558 mL
5 mM 0.3871 mL 1.9356 mL 3.8712 mL
10 mM — — —

*

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: ≥ 0.5 mg/mL (0.97 mM); Clear solution

    此方案可获得 ≥ 0.5 mg/mL (0.97 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 5.0 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% corn oil

    Solubility: ≥ 0.5 mg/mL (0.97 mM); Clear solution

    此方案可获得 ≥ 0.5 mg/mL (0.97 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 5.0 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 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Hoffmann E, et al. Pharmacokinetics and tolerability of SRT2104, a first-in-class small molecule activator of SIRT1, after single and repeated oral administration in man.

    [2]. Jiao D, et al. MicroRNA-34a targets sirtuin 1 and leads to diabetes-induced testicular apoptotic cell death. J Mol Med (Berl). 2018 Sep;96(9):939-949.

    [3]. Jiang M, et al. Sirtuin 1 activator SRT2104 protects Huntington’s disease mice. Ann Clin Transl Neurol. 2014 Dec;1(12):1047-52.

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