SRT1720 HCl

SRT1720 HCl是一种选择性的SIRT1激活剂,无细胞试验中EC50为0.16 μM,对SIRT2和SIRT3的作用弱230倍以上。SRT1720 还可诱导自噬。

SRT1720 HCl Chemical Structure

SRT1720 HCl Chemical Structure

CAS: 1001645-58-4

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 1960.55 现货
5mg RMB 1400.82 现货
50mg RMB 7964.73 现货
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客户使用Selleck的SRT1720 HCl发表文献176

产品质控

批次: 纯度: 99.61%
98.80

常与SRT1720 HCl一起在实验中被使用的化合物

Selisistat (EX 527)


SRT1720增加Pgrcre/+Rosa26mTmG/+小鼠的子宫内膜异位病变,而Selisistat显着减少子宫内膜异位病变的数量。

Kim TH, et al.J Clin Endocrinol Metab. 2022 Feb 17;107(3):788-800.

Resveratrol


SRT1720增强依托泊苷和长春新碱诱导的细胞死亡,而Resveratrol则抑制ES细胞中的细胞死亡。

Sonnemann J, et al. J Cancer Res Clin Oncol. 2016 Jan;142(1):17-26.

Quercetin


Quercetin在对抗D-GalN/LPS对雄性Wistar大鼠的细胞毒性作用方面比SRT1720更有效。

Kemelo MK, et al. Eur Rev Med Pharmacol Sci. 2016;20(2):363-71.

Astragaloside IV


SRT1720 HCl和Astragaloside IV在calpain-1敲除中对血管内皮功能障碍(VED)表现出相似的作用。

Zhao F, et al. Front Pharmacol. 2022 Aug 2;13:920977.

MDL-28170


SRT1720 HCl和MDL-28170治疗可恢复人冠状动脉内皮细胞(HCAEC)中线粒体ROS水平的增加和膜电位的降低。

Zhao F, et al. Front Pharmacol. 2022 Aug 2;13:920977.

SRT1720 HCl相关产品

相关信号通路图

Sirtuin抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
MC3T3-E1 Function Assay 10 μM 60 min  attenuates the FGF-2-induced osteoprotegerin mRNA expression 25290095
MC3T3-E1 Function Assay 10 μM 60 min  suppresses the FGF-2-stimulated osteoprotegerin release 25290095
MDA-MB-231 Function Assay 5 μM 16 h induces lysosomal membrane permeabilization 25411356
MDA-MB-231 Function Assay 5 μM 8 h increases the number of acidic vesicular organelles 25411356
Neu Growth Inhibition Assay 0-20 μM 24 h reduces cell viability dose dependently 25411356
HCT116 Growth Inhibition Assay 0-20 μM 24 h reduces cell viability dose dependently 25411356
A459 Growth Inhibition Assay 0-20 μM 24 h reduces cell viability dose dependently 25411356
BT20 Growth Inhibition Assay 0-20 μM 24 h reduces cell viability dose dependently 25411356
HS578T Growth Inhibition Assay 0-20 μM 24 h reduces cell viability dose dependently 25411356
SUM149 Growth Inhibition Assay 0-20 μM 24 h reduces cell viability dose dependently 25411356
MDA-MB-231 Growth Inhibition Assay 0-20 μM 24 h reduces cell viability dose dependently 25411356
SKBR3 Growth Inhibition Assay 0-20 μM 24 h reduces cell viability dose dependently 25411356
T47D Growth Inhibition Assay 0-20 μM 24 h reduces cell viability dose dependently 25411356
MCF-7 Growth Inhibition Assay 0-20 μM 24 h reduces cell viability dose dependently 25411356
MCF10A Growth Inhibition Assay 0-20 μM 24 h reduces cell viability dose dependently 25411356
RAW264.7 Function Assay 1 μM 6 h upregulates the reduced SIRT1 protein or mRNA levels by high glucose 25793995
NRK-49F Function Assay 0–2 μM 36 h enhances STAT3 phosphorylation 26022003
NRK-49F Function Assay 0–2 μM 36 h enhances phosphorylation of EGFR and PDGFRβ  26022003
NRK-49F Function Assay 0–2 μM 36 h increases expression of α-SMA and fibronectin dose dependently 26022003
SK-N-MC  Function Assay 3 μM 0-24 h activates caspase 3/7 26055805
SK-ES-1 Function Assay 10 μM 0-24 h activates caspase 3/7 26055805
WE-68 Function Assay 20 μM 0-24 h activates caspase 3/7 26055805
SK-N-MC  Apoptosis Assay 0-2.5 μM 24 h induces cell death in dose dependently 26055805
SK-ES-1 Apoptosis Assay 0-10 μM 24 h induces cell death in dose dependently 26055805
WE-68 Apoptosis Assay 0-24 μM 24 h induces cell death in dose dependently 26055805
MC3T3-E1 Function Assay 20 μM 1 h suppresses the TGF-β-induced phosphorylation of p44/p42 MAP kinase or SAPK/JNK 26136978
MC3T3-E1 Function Assay 10 µM  12 h reduces the VEGF mRNA expression levels stimulated by TGF-β 26136978
MC3T3-E1 Function Assay 10 µM  1 h reduces the TGF-β-stimulated VEGF release in dose- and time-dependent manner  26136978
CACs  Function Assay 4 μM 30 min induces acute SIRT1 activation  26254104
MC3T3-E1 Function Assay 10 μM 60 min  attenuates the FGF-2-induced osteoprotegerin mRNA expression 25290095
MC3T3-E1 Function Assay 10 μM 60 min  suppresses the BMP-4-stimulated VEGF release 24435444
MC3T3-E1 Function Assay 10 μM 60 min  suppresses the PGF2α-stimulated OPG release 24333336
MC3T3-E1 Function Assay 10 μM 60 min  reduces the PGF2α-stimulated phosphorylation of p44/p42 MAP kinase 24333336
MC3T3-E1 Function Assay 10 μM 60 min  attenuates the PGF2α-induced phosphorylation of both MEK1/2 and Raf-1 24333336
RPE Cell Viability Assay 5 µM 1 h attenuates OAβ-induced decrease of cell viability 24036938
9607 Cell Viability Assay 1 μM 36 h increases the cell viability compared with melatonin alone 23726949
9607 Function Assay 1 μM 36 h increases SIRT1 and decreased acetylated-p53 expression 23726949
RPMI.8226 Cell Viability Assay 7/10 μM 24 h decreases viability concentration dependently 21950728
U266 Cell Viability Assay 7/10 μM 24 h decreases viability concentration dependently 21950728
MM.1S Cell Viability Assay 7/10 μM 24 h decreases viability concentration dependently 21950728
KMS12 Cell Viability Assay 7/10 μM 24 h decreases viability concentration dependently 21950728
LR5 Cell Viability Assay 7/10 μM 24 h decreases viability concentration dependently 21950728
MM.1R Cell Viability Assay 7/10 μM 24 h decreases viability concentration dependently 21950728
Ina6 Cell Viability Assay 7/10 μM 24 h decreases viability concentration dependently 21950728
RPMI-8226 Apoptosis Assay 7/10 μM 24 h induces a significant increase in the Annexin V+/PI− apoptosis 21950728
MM.1R  Apoptosis Assay 7/10 μM 24 h induces a significant increase in the Annexin V+/PI− apoptosis 21950728
H411EC3 Function Assay 50/100 nM 6 h increases SIRT1 activity in the presence of TSA, PEPCK activity, mRNA levels of Pck1 and Pgc1α, and elevating glucose production 21212096
hepatocytes Function Assay 10 nM 6 h increases SIRT1 activity in the presence of TSA, PEPCK activity, mRNA levels of Pck1 and Pgc1α, and elevating glucose production 21212096
hepatocytes Function Assay 10 nM 6 h increases Hmgcr and Acc gene expression 21212096
U2OS Function assay 0.10 uM Activation of SIRT1 in human U2OS cells assessed as decrease in p53 deacetylation level at 0.10 uM 18046409
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
点击查看更多细胞系数据

生物活性

产品描述 SRT1720 HCl是一种选择性的SIRT1激活剂,无细胞试验中EC50为0.16 μM,对SIRT2和SIRT3的作用弱230倍以上。SRT1720 还可诱导自噬。
靶点
SIRT1 [1]
(Cell-free assay)
0.16 μM(EC50)
体外研究(In Vitro)
体外研究活性 SRT1720抗最近的乙酰化酶同系物SIRT2 (EC1.5为37 μM)和SIRT3 (EC1.5 > 300 μM)的最大激活率达781%。SRT1720在氨基末端催化区的变构位点结合到SIRT1酶-肽底物复合物上,降低乙酰化底物的米氏常数值。用SRT1720处理一周后,饲喂的葡萄糖水平降低,处理三周后,饲喂的葡萄糖水平进一步降低,持续处理10周。Rosiglitazone激活PPARγ,已经用于治疗II型糖尿病;而与Rosiglitazone相比,在进行腹膜葡糖糖耐量试验时,用SRT1720处理导致葡萄糖明显降低。SRT1720对用无糖食物喂养的鼠没有作用效果,显示出药理学SIRT1的激活不会产生低血糖。与Rosiglitazone相似,用SRT1720处理4周,明显降低高胰岛素血症,使升高的胰岛素水平恢部分复正常SRT1720处理腓肠肌,通过测定柠檬酸合酶活性发现线粒体各项能力上升15%。[1]高浓度 SRT1720 (15 μM)诱导正常细胞活力轻微下降,约10-20%。SRT1720明显抑制VEGF依赖的 MM 细胞迁移。[2]
激酶实验 SIRT1荧光偏振实验
在SIRT1 FP试验中,使用从p53序列中得到的含20个氨基酸的肽段 (Ac-Glu-Glu-Lys(biotin)-Gly-Gln-Ser-Thr-Ser-Ser-His-Ser-Lys(Ac)-Nle-Ser-Thr-Glu-Gly-Lys(MR121或 Tamra)-Glu-Glu-NH2)。肽段N端与生物素相连,C端用荧光标记修饰。监测酶活的反应是酶活偶联反应,第一步反应为SIRT1催化的脱乙酰反应,第二步反应为在新暴露的赖氨酸残基处进行胰蛋白酶催化的分裂。为了突出底物和产物的多种区别,加入链酶亲和素,反应终止。FP测试的敏感性可用来鉴定SRT1720。进行荧光偏振反应环境如下:0.5 μM 肽底物, 150 μM βNAD+, 0-10 nM SIRT1, 25 mM Tris-醋酸盐(pH 为8), 137 mM Na-Ac, 2.7 mM K-Ac, 1 mM Mg-Ac, 0.05% Tween-20, 0.1% Pluronic F127, 10 mM CaCl2, 5 mM DTT, 0.025% BSA, 及0.15 mM烟碱。 反应在37oC温育,加入烟碱终止反应,加入胰蛋白酶分裂脱乙酰底物。加入链酶亲和素在37oC温育。在650 nm 和680nm 处测定荧光偏振。
细胞实验 细胞系 人类血管内皮细胞(HUVECs)
浓度 5 μM
孵育时间 2小时
方法 使用Transwell迁移实验测定迁移率。通过基底膜的毛细血管样管结构形成试剂盒检测体外血管生成。用于内皮血管生成实验,从Clonetics获得的人类血管内皮细胞(HUVEC),保存在含5% FBS的内皮细胞生长培养基中。使用台盼蓝拒染法测定HUVEC细胞活力,观察到用SRT1720处理的细胞死亡率小于5%。
实验图片 检测方法 检测指标 实验图片 PMID
Western blot Cleaved-PARP-1 / Cleaved-caspase-3 / LC3-II / p62 / SIRT1 26655844
Immunofluorescence Cathepsin B 26655844
Growth inhibition assay Cell viability 25411356
体内研究(In Vivo)
体内研究活性 在DIO鼠中实施摄热量限制包括改善胰岛素敏感性,使葡萄糖和胰岛素水平维持正常,及提高线粒体能力后,可观察到SRT1720模拟一些功能。此外,在饮食导致的肥胖和遗传肥胖鼠中,SRT1720提高胰岛素敏感性,降低血浆葡萄糖,及提高线粒体能力。因此,SRT1720是有前途的新型治疗剂,可用于治疗像II型糖尿病之类的疾病。与提高的葡萄糖耐量相一致,在SRT1720处理的fa/fa鼠中,维持血糖正常所需的葡萄糖注入率(GIR)大约为35%, 全部的葡萄糖处理效率提高大约为20%。 [1] SRT1720作用于动物肿瘤模型研究时,抑制多发性骨髓瘤生长。SRT1720提高Bortezomib或Dexamethasone的毒性。[2]
动物实验 Animal Models 携带MM.1S细胞的Chase-SCID鼠
Dosages 200 mg/kg
Administration 口服处理

化学信息&溶解度

分子量 506.02 分子式

C25H23N7OS.HCl

CAS号 1001645-58-4 SDF Download SRT1720 HCl SDF
Smiles C1CN(CCN1)CC2=CSC3=NC(=CN23)C4=CC=CC=C4NC(=O)C5=NC6=CC=CC=C6N=C5.Cl
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 100 mg/mL ( 197.62 mM; DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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常见问题及建议解决方法

问题 1:
How can we prepare Srt1720 for in vivo mouse studies?

回答:
SRT1720 HCl can be dissolved in 30% PEG 400+0.5% Tween 80+5% Propylene glycol at 30mg/ml as a suspension. It is fine for oral gavage. And we’ve also found that it can be dissolved in 2% DMSO+30% PEG 300+1%Tween 80+ddH2O at 3mg/ml clearly, which could be used for injection. When prepare the solution, please dissolve the compound in DMSO clearly first, then add PEG and Tween. After they mixed well, dilute with water.

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