SRT 1720 is a selective activator of human SIRT1 with an EC1.5 of 0.16 μM, and shows less potent activities for SIRT2 and SIRT3 with EC1.5s of 37 μM and > 300 μM, respectively.
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SRT 1720 Chemische Struktur
CAS. Nr. : 925434-55-5
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SRT1720 rescues the downregulation of SIRT1 activity and protein expression in the aortas of KL+/– mice. A, Representative Western blot bands of Acetyl-P53 and total P53 and the quantification of SIRT1 activity. Data are expressed as the ratio of acetyl-p53/total P53. B, Representative Western blot bands and quantitative analysis of SIRT1 protein expression in aortas. Protein expression is normalized to β-actin, and the relative expression calculated as the fold change relative
SRT 1720 purchased from MedChemExpress. Usage Cited in:
Toxicol Lett. 2016 Dec 15;264:1-11.
[Abstract]
The HNF1α, FXR, Mrp2 and Bsep protein levels are decreased after EE administration and significantly increased by SRT1720 in a dose dependent manner, which is in accordance with the mRNA levels.
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Beschreibung
SRT 1720 is a selective activator of human SIRT1 with an EC1.5 of 0.16 μM, and shows less potent activities for SIRT2 and SIRT3 with EC1.5s of 37 μM and > 300 μM, respectively.
IC50 & Target[1][1]
SIRT1
0.16 μM (EC1.5)
SIRT2
37 μM (EC1.5)
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
SRT 1720 Related Antibodies
In Vivo
SRT 1720 (10, 30, 100 mg/kg, p.o.) significantly reduces the hyperinsulinaemia 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 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Room temperature in continental US; may vary elsewhere.
Speicherung
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
1 year
-20°C
6 months
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 41.67 mg/mL (88.74 mM; ultrasonic and warming and adjust pH to 2 with HCl and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
1 mM
2.1297 mL
10.6483 mL
21.2965 mL
5 mM
0.4259 mL
2.1297 mL
4.2593 mL
10 mM
0.2130 mL
1.0648 mL
2.1297 mL
View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Protocol 1
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly.
It is recommended to prepare fresh solutions and use them promptly within a short period of time. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution.
If precipitation or phase separation occurs during preparation,
heat and/or sonication can be used to aid dissolution.
Protocol 1
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 25 mg/mL (53.24 mM); Clear solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
[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
[Content Brief]
[2]. Baur JA, et al. Are sirtuins viable targets for improving healthspan and lifespan? Nat Rev Drug Discov. 2012 Jun 1;11(6):443-61
[Content Brief]
[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.
[Content Brief]
[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.
[Content Brief]
Tierverwaltung
[1]
Mice: Nine week old C57BL/6 male mice are fed a high fat diet (60% calories from fat) until their mean body weight reach 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 measure is 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 comparison to control using a Dunnett’s Test. A p value < 0.05 indicates a significant difference between groups.
MCE hat die Genauigkeit dieser Methoden nicht unabhängig bestätigt. Sie dienen nur als Referenz.
Verweise
[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
[Content Brief]
[2]. Baur JA, et al. Are sirtuins viable targets for improving healthspan and lifespan? Nat Rev Drug Discov. 2012 Jun 1;11(6):443-61
[Content Brief]
[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.
[Content Brief]
[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.
[Content Brief]
[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]. Baur JA, et al. Are sirtuins viable targets for improving healthspan and lifespan? Nat Rev Drug Discov. 2012 Jun 1;11(6):443-61
[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.
Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Optional Solvent
ConcentrationSolventMass
1 mg
5 mg
10 mg
25 mg
DMSO
1 mM
2.1297 mL
10.6483 mL
21.2965 mL
53.2413 mL
5 mM
0.4259 mL
2.1297 mL
4.2593 mL
10.6483 mL
10 mM
0.2130 mL
1.0648 mL
2.1297 mL
5.3241 mL
15 mM
0.1420 mL
0.7099 mL
1.4198 mL
3.5494 mL
20 mM
0.1065 mL
0.5324 mL
1.0648 mL
2.6621 mL
25 mM
0.0852 mL
0.4259 mL
0.8519 mL
2.1297 mL
30 mM
0.0710 mL
0.3549 mL
0.7099 mL
1.7747 mL
40 mM
0.0532 mL
0.2662 mL
0.5324 mL
1.3310 mL
50 mM
0.0426 mL
0.2130 mL
0.4259 mL
1.0648 mL
60 mM
0.0355 mL
0.1775 mL
0.3549 mL
0.8874 mL
80 mM
0.0266 mL
0.1331 mL
0.2662 mL
0.6655 mL
SRT 1720 Related Classifications
Help & FAQs
Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.