SRT 1720 Hydrochloride 是选择性的和具有口服活性的SIRT1激活剂,EC50为 0.10 μM,对 SIRT2 和 SIRT3 的作用较弱。
生物活性 | SRT 1720 Hydrochloride is a selective and orally active activator ofSIRT1with anEC50of 0.10 μM, and shows less potent activities onSIRT2andSIRT3[1]. |
IC50& Target[1] | SIRT1 0.10 μM (EC50) | SIRT1 0.16 μM (EC1.5) | SIRT2 37 μM (EC1.5) |
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体外研究 (In Vitro) | SRT 1720 effectively decreases the acetylation of p53 in cells even in the absence of SIRT1, and this is attributed to inhibition of histone acetyltransferase p300[2].
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体内研究 (In Vivo) | SRT 1720 (10, 30, 100 mg/kg, p.o.) treatment significantly reduces fasting blood glucose to near normal levels inLepob/obmice[1]. SRT 1720 has ability to protect against the negative effects of diet-induced obesity in mice, and has a connection to metabolic adaptation in fatty acid and oxidative metabolism through downstream targets of SIRT1 such as PGC1α and FOXO1[2]. SRT 1720 (50-100 mg/kg, p.o.), during emphysema development attenuates elastase-induced airspace enlargement and lung function impairment as well as reduces arterial oxygen saturation in WT mice[3].
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
溶解性数据 | In Vitro: DMSO : 62.5 mg/mL(123.51 mM;Need ultrasonic) H2O : 15.7 mg/mL(31.03 mM;Need ultrasonic and warming) 配制储备液 1 mM | 1.9762 mL | 9.8810 mL | 19.7621 mL | 5 mM | 0.3952 mL | 1.9762 mL | 3.9524 mL | 10 mM | 0.1976 mL | 0.9881 mL | 1.9762 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 (stored under nitrogen)。-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: 0.5% HPMC 0.2%Tween80 Solubility: 10 mg/mL (19.76 mM); Suspened solution; Need ultrasonic 2. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (4.11 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.11 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 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。 3. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (4.11 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.11 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 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。 4. 请依序添加每种溶剂: 5% DMSO 40%PEG300 5%Tween-80 50% saline Solubility: ≥ 1 mg/mL (1.98 mM); Clear solution 5. 请依序添加每种溶剂: 5% DMSO 95% (20%SBE-β-CDin saline) Solubility: ≥ 1 mg/mL (1.98 mM); Clear solution
*以上所有助溶剂都可在本网站选购。 |