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CAS No.: 2070015-26-6

Sirtuin modulator 1/SRT3025盐酸 Catalog No. CSN18940

Synonyms: SRT 3025 (hydrochloride);Sirtuin Modulator 1;SRT-3025

SRT3025 HCl is an orally available sirtuin modulator.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述SRT3025 is a Sirt1 inhibitor which showed effect on various fields including atheroprotection. Treatment with SRT3025 at concentration of 5μM and 10μM for 24h could attenuate Pcsk9 secretion and its binding to Ldlr in cultured AML12 hepatocytes. And this reduced Pcsk9-mediated Ldlr degradation and increased Ldlr expression and LDL uptake in vitro. This effect could also observed in vivo as administration of SRT3025 for 12 weeks through supplement in diet at 3.18g/kg diet could decrease plasma levels of LDL-cholesterol and total cholesterol and reduce atherosclerosis of Apoe^-/- mice fed a high-cholesterol diet (1.25% w/w). In addition, administration of SRT3025 increased deacetylation of hepatic p65 and skeletal muscle Foxo1. Exposure of SRT3025 at concentration below 5μM for 72h reduced viability of SU86.86 in a dose-dependent manner with IC50 of 0.98μM. Oral gavage with SRT3025 at dose of 50–200 mg/kg daily for 10 days prevented pancreatic tumor growth of mice subcutaneously xenograft Panc1 cells. The SRT3025-induced cell apoptosis in vitro was lysosomal dependent. Activation of Sirt1 by SRT3025 at concentration of 10μM inhibited murine osteoclast progenitor proliferation and reduced osteoclastogenesis, which was mediated by deacetylation of FoxOs. SRT3025 could increase the expression of the FoxO-target genes catalase and HO-1 in osteoclast progenitors in FoxO-dependent manner.
动物研究
剂量
Mice: 50 mg/kg - 200 mg/kg^[1] (p.o.)

给药途径
p.o.
临床研究

动物研究
剂量	Mice: 50 mg/kg - 200 mg/kg^[1] (p.o.)
给药途径	p.o.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01340911	Diabetes Mellitus, Type 2	Phase 1	Completed	-	United Kingdom ... more >> GSK Investigational Site Harrow, Middlesex, United Kingdom, HA1 3UJ Collapse <<

参考文献

[1] Chini CC, Espindola-Netto JM, et al. SIRT1-Activating Compounds (STAC) Negatively Regulate Pancreatic Cancer Cell Growth and Viability Through a SIRT1 Lysosomal-Dependent Pathway. Clin Cancer Res. 2016 May 15;22(10):2496-507.
[2] Zhang QS, Deater M, et al. The Sirt1 activator SRT3025 expands hematopoietic stem and progenitor cells and improves hematopoiesis in Fanconi anemia mice. Stem Cell Res. 2015 Jul;15(1):130-40.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.6496 mL
- 8.2481 mL
- 16.4962 mL
- 5 mM
- 0.3299 mL
- 1.6496 mL
- 3.2992 mL
- 10 mM
- 0.1650 mL
- 0.8248 mL
- 1.6496 mL

技术信息

CAS号

2070015-26-6

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C31H32ClN5O2S2

运输

蓝冰

分子量

606.20

别名

SRT 3025 (hydrochloride);Sirtuin Modulator 1;SRT-3025;SRT3025 HCl;SRT3025 hydrochloride

溶解度

DMSO	25.0 mg/mL (41.2 mM)
Water	insoluble

动物实验配方

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Sirtuin modulator 1/SRT3025盐酸 Catalog No. CSN18940

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