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SRT 1720

SRT 1720

产品编号 T5096   CAS 925434-55-5
别名: N-[2-[3-(1-哌嗪基甲基)咪唑并[2,1-B]噻唑-6-基]苯基]-2-喹喔啉甲酰胺

SRT 1720 是人 SIRT1 的选择性激活剂 ,EC1.5为 0.16 μM,对 SIRT2 和 SIRT3 的效力要低 230 倍以上。

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SRT 1720 Chemical Structure
SRT 1720, CAS 925434-55-5
规格 价格/CNY 货期 数量
1 mg ¥ 490 现货
2 mg ¥ 733 现货
5 mg ¥ 1,220 现货
10 mg ¥ 1,550 现货
25 mg ¥ 2,990 现货
50 mg ¥ 4,390 现货
100 mg ¥ 6,220 现货
1 mL * 10 mM (in DMSO) ¥ 2,150 现货
产品目录号及名称: SRT 1720 (T5096)
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纯度: 99.7%
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生物活性
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存储 & 溶解度
参考文献
产品描述 SRT 1720 is a selective activator of human SIRT1 (EC1.5: 0.16 μM) and is >230-fold less potent for SIRT2 and SIRT3.
靶点活性 SIRT1:0.16 μM (EC1.5, cell free), SIRT2:37 μM (EC1.5, cell free)
体外活性 The maximum activation ratio of SRT1720 versus the closest sirtuin homologs, SIRT2 (EC1.5 = 37 μM) and SIRT3 (EC1.5 > 300 μM) is up to 781%. SRT1720 binds to the SIRT1 enzyme-peptide substrate complex at an allosteric site amino-terminal to the catalytic domain and lower the Michaelis constant for acetylated substrates. Higher concentrations of SRT1720 (15 μM) induces a modest (10-20%) decrease in normal cell viability. SRT1720 also significantly inhibits VEGF-dependent MM cell migration [1].
体内活性 SRT 1720 (10, 30, 100 mg/kg, p.o.) significantly reduces the hyperinsulinemia after 4 weeks, partially normalizing elevated insulin levels similar to rosiglitazone treatment. SRT 1720 treatment significantly reduces fasting blood glucose to near normal levels in Lepob/ob mice[1]. SRT 1720 has the 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].
动物实验 Nine-week-old C57BL/6 male mice are fed a high-fat diet (60% calories from fat) until their mean body weight reaches approximately 40 g. The mice are then divided into test groups (6-10 per group). SRT1460 (100 mg/kg), SRT1720 (100 mg/kg), SRT501 (500 mg/kg) and rosiglitazone (5 mg/kg) are administered once daily via oral gavage. The vehicle used is 2% HPMC + 0.2% DOSS. Individual mouse body weights are measured twice weekly. At 2, 4, 6, 8 and 10 weeks of dosing a fed blood glucose measurement are taken and after 5 weeks of treatment, an IPGTT is conducted on all mice from each of the groups. After 10 weeks of treatment, an ITT is conducted. Statistical analysis is completed using the JMP program. Data are analyzed by a one way ANOVA with a comparison to control using a Dunnett's Test. A p-value < 0.05 indicates a significant difference between groups.
别名 N-[2-[3-(1-哌嗪基甲基)咪唑并[2,1-B]噻唑-6-基]苯基]-2-喹喔啉甲酰胺
分子量 469.56
分子式 C25H23N7OS
CAS No. 925434-55-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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TargetMol Library Books参考文献

1. Milne JC et al. Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes. Nature. 2007 Nov 29;450(7170):712-6 2. Chauhan D, et al. Preclinical evaluation of a novel SIRT1 modulator SRT1720 in multiple myeloma cells. Br J Haematol. 2011 Dec;155(5):588-98. 3. Yao H, et al. SIRT1 protects against emphysema via FOXO3-mediated reduction of premature senescence in mice.,J Clin Invest. 2012 Jun 1;122(6):2032-45. 4. Yu L, et al. Protective effects of SRT1720 via the HNF1α/FXR signalling pathway and anti-inflammatory mechanisms in mice with estrogen-induced cholestatic liver injury. Toxicol Lett. 2016 Dec 15;264:1-11. 5. Wu Q, Hu Y, Jiang M, et al. Effect of Autophagy Regulated by Sirt1/FoxO1 Pathway on the Release of Factors Promoting Thrombosis from Vascular Endothelial Cells[J]. International journal of molecular sciences. 2019, 20(17): 4132.

TargetMol Library Books文献引用

1. Wu Q, Hu Y, Jiang M, et al. Effect of Autophagy Regulated by Sirt1/FoxO1 Pathway on the Release of Factors Promoting Thrombosis from Vascular Endothelial Cells. International journal of molecular sciences. 2019, 20(17): 4132. 2. Lian L, Le Z, Wang Z, et al.SIRT1 Inhibits High Glucose–Induced TXNIP/NLRP3 Inflammasome Activation and Cataract Formation.Investigative Ophthalmology & Visual Science.2023, 64(3): 16-16. 3. Li L, Fu S, Wang J, et al.SRT1720 inhibits bladder cancer cell progression by impairing autophagic flux.Biochemical Pharmacology.2024: 116111.
B2 PROTAC Sirt2 Degrader-1 SPC-180002 MIND4-19 BML-278 SIRT1 activator 1 3-TYP SIRT-IN-2

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 已知活性化合物库 表观遗传库 自噬库 抗糖尿病库 NO PAINS 化合物库 DNA 损伤和修复分子库 抗代谢疾病化合物库 抗衰老化合物库 经典已知活性库

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Keywords

SRT 1720 925434-55-5 Autophagy Chromatin/Epigenetic DNA Damage/DNA Repair Sirtuin N-[2-[3-(1-哌嗪基甲基)咪唑并[2,1-B]噻唑-6-基]苯基]-2-喹喔啉甲酰胺 inhibit Inhibitor SRT1720 SRT-1720 inhibitor

 

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