SRT1720 HCl (Synonyms: SRT-1720,SRT 1720,SRT 1720 Hydrochloride) |
| Catalog No.GC17101 |
SRT1720 HCl is an activator of SIRT1 (EC1.5 = 0.16 µM and maximum activation = 781%), a NAD+-dependent protein and histone deacetylase that plays an important role in numerous biologic processes.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1001645-58-4
Sample solution is provided at 25 µL, 10mM.
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SRT1720 HCl is an activator of SIRT1 (EC1.5 = 0.16 µM and maximum activation = 781%) [1], a NAD+-dependent protein and histone deacetylase that plays an important role in numerous biologic processes [2]. SRT1720 HCl also inhibited p300 activity with IC50 of 9 µM [3].
SRT1720 HCl treatment decreased the expression of lipogenic genes in HepG2 cells [4]. The viability of MDA-MB-231 and BT20 basal-type breast cancer cells decreased by more than 80% with 5 µM of SRT1720 HCl, whereas the viability of MCF-7 luminal-type cells only decreased by 20% with 20 µM of treatment. After SRT1720 HCl (5 µM, 8h) treatment, 1% of the MDA-MB-231 cells were positive for early apoptosis and 12% of the cells were positive for late apoptosis/necrosis [2].
SRT1720 HCl (200 mg/kg for 10 wk) reduced fat accumulation in the liver and ameliorated liver dysfunction in MSG mice. The administration of SRT1720 HCl to MSG mice for 10 wk reduced fat accumulation by 21%. The serum levels of aminotransferases were also elevated in MSG mice. Administration of SRT1720 HCl improved dyslipidemia in MSG mice [4]. Administration of SRT1720 HCl (100 mg/kg) reduced fed glucose levels after 1 week of treatment that continued through 10 weeks of dosing in diet-induced obesity (DIO) mice [5].
References:
[1]. Milne J C, Lambert P D, Schenk S, et al. Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes[J]. Nature, 2007, 450(7170): 712-716.
[2]. Lahusen T J, Deng C X. SRT1720 Induces Lysosomal-Dependent Cell Death of Breast Cancer CellsSRT1720 Induces Lysosomal-Dependent Cell Death[J]. Molecular cancer therapeutics, 2015, 14(1): 183-192. SRT1720 treatment decreased the expression of lipogenic genes in HepG2 cells.
[3]. Huber J L, McBurney M W, DiStefano P S, et al. SIRT1-independent mechanisms of the putative sirtuin enzyme activators SRT1720 and SRT2183[J]. Future medicinal chemistry, 2010, 2(12): 1751-1759.
[4]. Yamazaki Y, Usui I, Kanatani Y, et al. Treatment with SRT1720, a SIRT1 activator, ameliorates fatty liver with reduced expression of lipogenic enzymes in MSG mice[J]. American Journal of Physiology-Endocrinology and Metabolism, 2009, 297(5): E1179-E1186.
| Cell experiment [1]: | |
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Cell lines |
MDA-MB-231 Breast cancer cells, BT20 basal-type breast cancer cells, MCF-7 luminal-type cells |
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Preparation Method |
MDA-MB-231 cells were plated at 15,000 cells/well in 24-well plates. The day after plating, SRT1720 HCl was added to the cells for the designated time and concentration. Cell viability was assessed by methylthiazolydiphenyl-tetrazolium bromide (MTT) assay. |
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Reaction Conditions |
0-20µM for 24 hours |
|
Applications |
The viability of MDA-MB-231 and BT20 basal-type breast cancer cells decreased by more than 80% with 5 µmol/L of SRT1720, whereas the viability of MCF-7 luminal-type cells only decreased by 20% with 20 µmol/L of treatment |
| Animal experiment [2]: | |
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Animal models |
male MSG mice and control male ICR mice |
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Preparation Method |
Twenty ICR mice and 12 MSG mice at 6 wk old were analyzed as pretreatment groups before starting SRT1720 HCl treatment. SRT1720 HCl was mixed with standard chow (200 mg.kg body wt-1.day-1) and orally administered to 6-wk-old MSG mice for 10 wk. Fifteen ICR mice, 15 MSG mice, and 15 MSG mice with SRT1720 HCl treatment at 16 wk old were analyzed as post treatment groups after a 10-wk treatment period. |
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Dosage form |
200 mg.kg body wt-1.day-1, oral |
|
Applications |
Administration of SRT1720 HCl reduced the acetylation level of PGC-1α almost to the control level, whereas it did not alter the expression of SIRT1 at either the mRNA or protein levels in the liver. The body weight and the weight of the epididymal fat in 16-wk-old MSG mice was higher than those in control mice by ∼20 and 60%, respectively. SRT1720 HCl treatment did not significantly affect the body weight or food intake of the MSG mice. |
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References: [1]: Lahusen T J, Deng C X. SRT1720 Induces Lysosomal-Dependent Cell Death of Breast Cancer CellsSRT1720 Induces Lysosomal-Dependent Cell Death[J]. Molecular cancer therapeutics, 2015, 14(1): 183-192. |
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| Cas No. | 1001645-58-4 | SDF | |
| Synonyms | SRT-1720,SRT 1720,SRT 1720 Hydrochloride | ||
| Chemical Name | N-[2-[3-(piperazin-1-ylmethyl)imidazo[2,1-b][1,3]thiazol-6-yl]phenyl]quinoxaline-2-carboxamide;hydrochloride | ||
| Canonical SMILES | C1CN(CCN1)CC2=CSC3=NC(=CN23)C4=CC=CC=C4NC(=O)C5=NC6=CC=CC=C6N=C5.Cl | ||
| Formula | C25H23N7OS.HCl | M.Wt | 506.02 |
| Solubility | 100 mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9762 mL | 9.881 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 |
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Quality Control & SDS
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- Purity: >98.00%
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