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SRT1720 hydrochloride

SRT1720 hydrochloride

产品编号 T2412   CAS 1001645-58-4
别名: SRT1720 HCl, SRT 1720 Hydrochloride

SRT1720 hydrochloride (SRT1720 HCl) 是 SIRT1(EC1.5: 0.16 μM) 的选择性激活剂,对 SIRT2/SIRT3 (EC1.5s: 37 μM/300 μM) 的活性较低。

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SRT1720 hydrochloride Chemical Structure
SRT1720 hydrochloride, CAS 1001645-58-4
规格 价格/CNY 货期 数量
1 mg ¥ 478 现货
2 mg ¥ 697 现货
5 mg ¥ 1,160 现货
10 mg ¥ 1,860 现货
25 mg ¥ 3,730 现货
50 mg ¥ 4,890 现货
100 mg ¥ 6,970 现货
200 mg ¥ 9,430 现货
500 mg ¥ 13,900 现货
1 mL * 10 mM (in DMSO) ¥ 1,630 现货
其他形式的 SRT1720 hydrochloride:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
产品目录号及名称: SRT1720 hydrochloride (T2412)
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选择批次  
纯度: 99.93%
纯度: 99.59%
纯度: 98.76%
纯度: 98%
纯度: 98%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 SRT1720 hydrochloride (SRT1720 HCl) is a selective activator of SIRT1 (EC1.5: 0.16 μM) and shows less potent activities on SIRT2/SIRT3 (EC1.5s: 37 μM/300 μM).
靶点活性 SIRT1:0.16 μM(EC1.5, cell free)
体外活性 SRT1720 is an activator of SIRT1 (EC1.5 = 0.16 μM and maximum activation = 781%). SRT1720 is selective for activation of SIRT1 versus the closest sirtuin homologues, SIRT2 and SIRT3 (SIRT2: EC1.5 = 37 μM; SIRT3: EC1.5 > 300 μM) [1].
体内活性 SRT1720 exhibited a pharmacokinetic profile suitable for in vivo evaluation in both mouse (bioavailability = 50%, terminal t1/2 = ~5 h, Area Under the Curve (AUC) = 7,892 ng h/ml/) and rat (bioavailability = 25%, terminal t1/2 = ~8.4 h, AUC = 3,714 ng/h/ml). In DIO mice, fasting blood glucose levels are elevated (120–150 mg dl?1 range) after being placed on a high-fat diet. Administration of SRT1720 reduced fed glucose levels after 1 week of treatment with further reduction after 3 weeks of treatment that continued through 10 weeks of dosing. Glucose excursion during an intraperitoneal glucose tolerance test was also significantly reduced in the SRT1720 group, and comparable to rosiglitazone, a PPARγ activator that has been used to treat type 2 diabetes [1]. SRT1720 attenuated stress-induced premature cellular senescence and protected against emphysema induced by cigarette smoke and elastase in mice [2]. In animal tumour model studies, SRT1720 inhibited MM tumour growth. SRT1720 enhanced the cytotoxic activity of bortezomib or dexamethasone [3].
激酶实验 In the SIRT1 FP assay, SIRT1 activity was monitored using a 20 amino acid peptide (AcGlu-Glu-Lys(biotin)-Gly-Gln-Ser-Thr-Ser-Ser-His-Ser-Lys(Ac)-Nle-Ser-Thr-Glu-Gly–Lys(MR121 or Tamra)-Glu-Glu-NH2) derived from the sequence of p53. The peptide was N-terminally linked to biotin and C-terminally modified with a fluorescent tag. The reaction for monitoring enzyme activity was a coupled enzyme assay where the first reaction was the deacetylation reaction catalyzed by SIRT1 and the second reaction was cleavage by trypsin at the newly exposed lysine residue. The reaction was stopped and streptavidin was added in order to accentuate the mass differences between substrate and product. In total, 290,000 compounds were screened and 127 hits were confirmed. The sensitivity of the FP assay allowed identification of compounds that exhibited low level activation of SIRT1 (≥17% activation at 20 μM) producing multiple classes of activators representing distinct structural classes. The fluorescence polarization reaction conditions were as follows: 0.5 μM peptide substrate, 150 μM βNAD+, 0-10 nM SIRT1, 25 mM Tris-acetate pH 8, 137 mM Na-Ac, 2.7 mM K-Ac, 1 mM Mg-Ac, 0.05% Tween-20, 0.1% Pluronic F127, 10 mM CaCl2, 5 mM DTT, 0.025% BSA, and 0.15 mM nicotinamide. The reaction was incubated at 37°C and stopped by addition of nicotinamide, and trypsin was added to cleave the deacetylated substrate. This reaction was incubated at 37°C in the presence of 1 μM streptavidin. Fluorescent polarization was determined at excitation (650 nm) and emission (680 nm) wavelengths [1].
细胞实验 Cell viability was assessed with a colorimetric assay using MTT as described previously. Apoptosis assay was quantified using Annexin V-FITC/Propidium iodide (PI) apoptosis detection kit, as per manufacturer's instructions, followed by analysis on FACS Calibur [3].
动物实验 Sirtinol (2 mg/kg) was administered by peritoneal injection, whereas SRT1720 (100 mg/kg) was administered through oral gavage 1 hour prior to CS exposure daily for 3 days. In a separate experiment, SRT1720 (25, 50, and 100 mg/kg) or PHA-408 (50 mg/kg) was dissolved in 0.5% carboxymethylcellulose containing 0.025% Tween 20 and injected via oral gavage into the conscious mice 24 hours prior to elastase administration, which was repeated daily (5 days per week) until 21 days after elastase administration. To study the therapeutic effect on emphysema, SRT1720 (100 mg/kg) was orally administered daily for 2 weeks after the development of elastase-induced emphysema [2].
别名 SRT1720 HCl, SRT 1720 Hydrochloride
化合物与蛋白结合的复合物

T2412_1

Structure of human SIRT3 in complex with SRT1720 inhibitor

分子量 506.22
分子式 C25H24ClN7OS
CAS No. 1001645-58-4

存储

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

溶解度

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 36 mg/mL (71.1 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9754 mL 9.8771 mL 19.7543 mL 49.3856 mL
5 mM 0.3951 mL 1.9754 mL 3.9509 mL 9.8771 mL
10 mM 0.1975 mL 0.9877 mL 1.9754 mL 4.9386 mL
20 mM 0.0988 mL 0.4939 mL 0.9877 mL 2.4693 mL
50 mM 0.0395 mL 0.1975 mL 0.3951 mL 0.9877 mL

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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. 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. 3. 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. 4. Su G, Yang W, Wang S, et al. SIRT1-autophagy axis inhibits excess iron-induced ferroptosis of foam cells and subsequently increases IL-1Β and IL-18[J]. Biochemical and Biophysical Research Communications. 2021, 561: 33-39. 5. Chen W, Lin B, Xie S, et al. Naringenin protects RPE cells from NaIO3-induced oxidative damage in vivo and in vitro through up-regulation of SIRT1[J]. Phytomedicine. 2020: 153375. 6. 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. Chen W, Lin B, Xie S, et al. Naringenin protects RPE cells from NaIO3-induced oxidative damage in vivo and in vitro through up-regulation of SIRT1. Phytomedicine. 2020: 153375 2. 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. 3. Su G, Yang W, Wang S, et al. SIRT1-autophagy axis inhibits excess iron-induced ferroptosis of foam cells and subsequently increases IL-1Β and IL-18. Biochemical and Biophysical Research Communications. 2021, 561: 33-39. 4. Ma Y, Ji Y, Xu L, et al. Obesity aggravated hippocampal-dependent cognitive impairment after sleeve gastrectomy in C57/BL6J mice via SIRT1/CREB/BDNF pathway. Experimental Brain Research. 2022: 1-10.
Ginkgolide C Sirt1/2-IN-2 SIRT5 inhibitor 6 SIRT5 inhibitor 5 Resveratrol E1231 SRT 1460 SIRT7 inhibitor 97491

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 DNA 损伤和修复分子库 染色质修饰分子库 NO PAINS 化合物库 临床前化合物库 抗代谢疾病化合物库 自噬库 抗衰老化合物库 谷氨酰胺代谢化合物库

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Keywords

SRT1720 hydrochloride 1001645-58-4 Chromatin/Epigenetic DNA Damage/DNA Repair Sirtuin SRT1720 HCl SRT-1720 Hydrochloride SRT-1720 hydrochloride SRT 1720 Hydrochloride SRT1720 Hydrochloride Inhibitor inhibitor inhibit

 

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