SRT 1720

Modify Date: 2024-01-10 08:31:27

SRT 1720 Structure
SRT 1720 structure
Common Name SRT 1720
CAS Number 925434-55-5 Molecular Weight 469.56100
Density 1.46 Boiling Point N/A
Molecular Formula C25H23N7OS Melting Point 221ºC
MSDS N/A Flash Point N/A

 Use of SRT 1720


SRT 1720 is a selective activator of human SIRT1 with an EC1.5 of 0.16 μM, and shows less potent activities agaiinst SIRT2 and SIRT3 with EC1.5s of 37 μM and > 300 μM, respectively.

 Names

Name N-[2-[3-(piperazin-1-ylmethyl)imidazo[2,1-b][1,3]thiazol-6-yl]phenyl]quinoxaline-2-carboxamide
Synonym More Synonyms

 SRT 1720 Biological Activity

Description SRT 1720 is a selective activator of human SIRT1 with an EC1.5 of 0.16 μM, and shows less potent activities agaiinst SIRT2 and SIRT3 with EC1.5s of 37 μM and > 300 μM, respectively.
Related Catalog
Target

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].
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].
Animal Admin 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.
References

[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.

 Chemical & Physical Properties

Density 1.46
Melting Point 221ºC
Molecular Formula C25H23N7OS
Molecular Weight 469.56100
Exact Mass 469.16800
PSA 115.69000
LogP 4.00320

 Safety Information

HS Code 2934100090

 Synthetic Route

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SRT 1720 Structure

SRT 1720

CAS#:925434-55-5

Literature: WO2008/156866 A1, ; Page/Page column 74 ; WO 2008/156866 A1

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SRT 1720 Structure

SRT 1720

CAS#:925434-55-5

Literature: Journal of Medicinal Chemistry, , vol. 52, # 5 p. 1275 - 1283

 Precursor & DownStream

Precursor  2

DownStream  0

 Customs

HS Code 2934100090
Summary 2934100090 other compounds containing an unfused thiazole ring (whether or not hydrogenated) in the structure VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:20.0%

 Synonyms

N-(2-(3-(piperazin-1-ylmethyl)imidazo[2,1-b]thiazol-6-yl)phenyl)quinoxaline-2-carboxamide
SRT 1720
Top Suppliers:I want be here
  • DC Chemicals Limited
  • China
  • Product Name: SRT1720
  • Price: $450.0/100mg $800.0/250mg $1500.0/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao


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Price: $132/5mg

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