SRT1720 HCl

CAS: 1001645-58-4 货号: S408503 分子式: C25H23N7OS.HCl 分子量: 506.02 PubChem CID: 25232708
有货
级别和纯度: 10mM in DMSO
储存条件
-80℃储存
运输条件
特低温运输
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规格
库存
价格
数量
1ml
S408503-1ml
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为什么选择此级别

,适用于对基线干扰要求严格的色谱和分析工作流程。

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储存与运输

-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。

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质量文档

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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。

概述

SRT1720是一种选择性的SIRT1激活剂,EC50为0.16 μM,比作用于SIRT2和SIRT3效果弱230倍以上。A selective SIRT1 activator

Information

SRT1720 HCl is a selectiveSIRT1activator withEC50of 0.16 μM in a cell-free assay, but is >230-fold less potent for SIRT2 and SIRT3. SRT1720 inducesautophagy.


In vitro

The maximum activation ratio of SRT1720 versus the closest sirtuin homologues, SIRT2 (EC1.5 = 37 μM) and SIRT3 (EC1.5 > 300 μM) is up to 781%. SRT1720 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. SRT1720 could reduce fed glucose levels. Glucose excursion during an intraperitoneal glucose tolerance test is also significantly reduced in the SRT1720 group, and comparable to rosiglitazone, a PPARγ activator that has been used to treat type 2 diabetes. SRT1720 does not have an effect on fasting glucose in chow-fed mice, revealing that pharmacological SIRT1 activation is unlikely to induce hypoglycaemia. SRT1720 significantly reduces the hyperinsulinaemia after 4 weeks, partially normalizing increased insulin levels similar to rosiglitazone treatment. SRT1720 treatment increases mitochondrial capacity by 15% in gastrocnemius muscle as measured by citrate synthase activity. Higher concentrations of SRT1720 (15 μM) induces a modest (10-20%) decrease in normal cell viability. SRT1720 also significantly inhibits VEGF-dependent MM cell migration.


In vivo

In DIO mice SRT1720 mimics several of the effects observed after calorie restriction including improved insulin sensitivity, normalized glucose and insulin levels, and increased mitochondrial capacity. In addition, in diet-induced obese and genetically obese mice, SRT1720 improves 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. Consistent with improved glucose tolerance, the glucose infusion rate required to maintain euglycaemia is approximately 35% higher in SRT1720-treated fa/fa rats, and the total glucose disposal rate is increased by approximately 20%. SRT1720 also prevents multiple myeloma tumor growth. SRT1720 increases the cytotoxic activity of bortezomib or dexamethasone.


Cell Data

cell lines:HCC827, H358, H460, HepG2, Hep3B2, Sk-Hep-1, Capan1, BxPc3, MCF-7, MDA-MB-231, and Sk-Br-3


Concentrations:5 μM


Incubation Time:2 hours


Powder Purity:≥97%


规格

英文别名
N-(2-(3-(piperazin-1-ylmethyl)imidazo[2,1-b]thiazol-6-yl)phenyl)quinoxaline-2-carboxamide hydrochloride
规格或纯度
10mM in DMSO
英文名称
SRT1720 HCl
生化机理
SRT1720 HCl 是一种选择性 SIRT1 激活剂,在无细胞试验中的 EC50 值为 0.16 μM,但对 SIRT2 和 SIRT3 的激活作用要低 230 倍以上。SRT1720 可诱导自噬。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
分子类型
小分子
Isomeric SMILES
C1CN(CCN1)CC2=CSC3=NC(=CN23)C4=CC=CC=C4NC(=O)C5=NC6=CC=CC=C6N=C5.Cl
PubChem CID
分子量
506.02

技术文档

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高级数据

化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 67 mg/mL (198.0 mM)
质检证书(CoA,COO,BSE/TSE 和分析图谱)
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常见问题

本产品应如何储存?
请于?80 °C条件下保存。需超低温保存以维持规定的有效期。
本产品如何运输?
本产品采用干冰配冷袋冷冻运输。收货后请立即拆包,并按上述储存条件保存;处理干冰时请戴隔热手套并保持通风。
本产品的 CAS 号、分子式和分子量是多少?
本产品的 CAS 号为 1001645-58-4,分子式为 C25H23N7OS.HCl,分子量为 506.02 g/mol。
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