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
CAS: 1001645-58-4
产品质控
批次：
纯度：
99.61%
99.61
常与SRT1720 HCl一起在实验中被使用的化合物
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.
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.
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。
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。
SRT1720 HCl相关产品
| 相关靶点 | SIRT1 SIRT2 SIRT3 SIRT6 SIRT5 | 点击展开 |
|---|---|---|
| 相关产品 | Selisistat (EX 527) Sirtinol Quercetin Fisetin 3-TYP AGK2 OSS_128167 SRT2104 (GSK2245840) SirReal2 Thiomyristoyl Salvianolic acid B SRT2183 UBCS039 Salermide SRT3025 HCl AK 7 NRD167 Inauhzin CAY10602 | 点击展开 |
| 相关化合物库 | 激酶抑制剂库 FDA药物库 天然产物库 已知活性药物库-I 高选择性抑制剂库 | 点击展开 |
相关信号通路图
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 |
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| 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。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。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] |
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|---|---|---|---|---|
| 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%。 |
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| 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。 |
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|---|---|---|
| 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) | |||
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体外溶解度 |
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 |
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体内溶解度 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
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
只
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，注：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：取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：取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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