Research Area
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SRT1720 Chemical Structure
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Biological Activity
SRT1720 is a selective activator of human SIRT1 (EC1.5 = 0.16 μM and maximum activation = 781%) versus the closest sirtuin homologues, SIRT2 and SIRT3，(SIRT2: EC1.5 = 37 μM；SIRT3: EC1.5 > 300 μM). This agent 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. [1]
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−1 ml−1) and rat (bioavailability = 25%, terminal t1/2 = ~8.4 h, AUC = 3,714 ng h−1 ml−1). [1]
In diet-induced obese and genetically obese mice, SRT1720 improved insulin sensitivity, lower plasma glucose, and increase mitochondrial capacity. Thus, SRT1720 is a promising new therapeutic agent for treating diseases of ageing such as type 2 diabetes. [1]
However, the claim that SRT-1720 is a SIRT1 activator has been questioned. [2,3]
References on SRT1720
- [1] Nature. 2007 Nov 29;450(7170):712-6.
- [2] J Biol Chem. 2010 Mar 12;285(11):8340-51.
- [3] Drug Des. 2009;74, 619–624
Chemical Information
| Molecular Weight (WM): | 506.02 |
|---|---|
| Formula: | C25H23N7OS.HCl |
| CAS No.: | 1001645-58-4 |
| Synonyms: |
SRT-1720
|
| Dissolve in (25°C): | DMSO ≥101mg/mL |
| Water ≥23mg/mL | |
| Ethanol <1mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
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Selleck's high quality products have been used in several published research findings, including the following:
Suberoylanilide Hydroxamic Acid (Vorinostat) Up-regulates Progranulin Transcription: rational therapeutic approach to frontotemporal dementia
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