SRT1720 HCl

製品コード：S1129 純度：99.61%

SRT1720 HCl is a selective SIRT1 activator with EC50 of 0.16 μM in a cell-free assay, but is >230-fold less potent for SIRT2 and SIRT3. SRT1720 induces autophagy.

CAS No. 1001645-58-4

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 35700	国内在庫あり
5mg	JPY 25500	国内在庫あり
50mg	JPY 145500	国内在庫あり
1g	JPY 598500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（177）

製品安全説明書

現在のバッチを見る：純度： 99.61%

99.61

SRT1720 HClと併用されることが多い化合物

Selisistat (EX 527)

SRT1720 increases endometriotic lesions in Pgrcre/+Rosa26mTmG/+ mice, while Selisistat significantly reduces the number of endometriotic lesions.

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

Resveratrol

SRT1720 enhances etoposide- and vincristine-induced cell death, while resveratrol inhibits it in ES cells.

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

Quercetin

Quercetin is more efficacious than SRT1720 in combatting the cytotoxic effects of D-GalN/LPS in Male Wistar rats.

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

Astragaloside IV

SRT1720 HCl and Astragaloside exhibit similar effects in calpain-1 knockout on Vascular endothelial dysfunction (VED).

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

MDL-28170

SRT1720 HCl and MDL-28170 treatment, including As-IV, restores the increased level of mitoROS and the reduced membrane potential in human coronary artery endothelial cells (HCAECs).

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

SRT1720 HCl関連製品

関連ターゲット	SIRT1 SIRT2 SIRT3 SIRT6 SIRT5	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Bioactive Compound Library-Ⅱ	もっと見る

シグナル伝達経路

Sirtuinシグナル伝達経路

Sirtuin阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
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
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生物活性

製品説明

SRT1720 HCl is a selective SIRT1 activator with EC50 of 0.16 μM in a cell-free assay, but is >230-fold less potent for SIRT2 and SIRT3. SRT1720 induces autophagy.

Targets

SIRT1 ^[1]
(Cell-free assay)

0.16 μM(EC50)

In Vitro
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. ^[1] 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. ^[2]
Kinase Assay	SIRT1 fluorescence polarization assay
Kinase Assay	In the SIRT1 FP assay, SIRT1 activity is monitored using a 20 amino acid peptide (Ac-Glu-Glu-Lys(biotin)-Gly-Gln-Ser-Thr-Ser-Ser-His-Ser-Lys(Ac)-Nle-Ser-Thr-Glu-Gly–Lys(MR121 or Tamra)-Glu-Glu-NH₂) derived from the sequence of p53. The peptide is N-terminally linked to biotin and C-terminally modified with a fluorescent tag. The reaction for monitoring enzyme activity is a coupled enzyme assay where the first reaction is the deacetylation reaction catalyzed by SIRT1 and the second reaction is cleavage by trypsin at the newly exposed lysine residue. The reaction is stopped and streptavidin is added in order to accentuate the mass differences between substrate and product. The sensitivity of the FP assay allows identification of SRT1720. The fluorescence polarization reaction conditions are as follows: 0.5 μM peptide substrate, 150 μM βNAD⁺, 0-10 nM SIRT1, 25 mM Tris-acetate pH 8, 137 mM Na-Ac, 2.7 mM K-Ac, 1 mM Mg-Ac, 0.05% Tween-20, 0.1% Pluronic F127, 10 mM CaCl 2, 5 mM DTT, 0.025% BSA, and 0.15 mM nicotinamide. The reaction is incubated at 37 °C and stopped by addition of nicotinamide, and trypsin is added to cleave the deacetylated substrate. This reaction is incubated at 37 °C in the presence of 1 μM streptavidin. Fluorescent polarization is determined at excitation (650 nm) and emission (680 nm) wavelengths.
細胞実験	細胞株	Human vascular endothelial cells (HUVECs)
	濃度	5 μM
	反応時間	2 hours
	実験の流れ	Transwell Insert Assays are utilized to measure migration. In vitro angiogenesis is assessed by Matrigel capillary-like tube structure formation assay. For endothelial tube formation assay, human vascular endothelial cells (HUVECs) are obtained from Clonetics and maintained in endothelial cell growth medium-2 containing 5% FBS. After three passages, HUVEC cell viability is measured with the trypan blue exclusion assay, and <5% of cell death is observed with SRT1720 treatment.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	Cleaved-PARP-1 / Cleaved-caspase-3 / LC3-II / p62 / SIRT1		26655844
	Immunofluorescence	Cathepsin B		26655844
	Growth inhibition assay	Cell viability		25411356

In Vivo
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%. ^[1] SRT1720 also prevents multiple myeloma tumor growth. SRT1720 increases the cytotoxic activity of bortezomib or dexamethasone. ^[2]
動物実験	動物モデル	Chase-SCID mice with MM.1S cells
	投与量	200 mg/kg
	投与経路	Orally

参考
[1] Milne JC, et al. Nature. 2007, 450(7170), 712-716. [2] Chauhan D, et al. Br J Haematol. 2011, 155(5), 588-598.

参考

化学情報

分子量	506.02	化学式	C₂₅H₂₃N₇OS.HCl
CAS No.	1001645-58-4	SDF	Download SRT1720 HCl SDFをダウンロードする
Smiles	C1CN(CCN1)CC2=CSC3=NC(=CN23)C4=CC=CC=C4NC(=O)C5=NC6=CC=CC=C6N=C5.Cl
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (197.62 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

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Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須

よくある質問（FAQ）

質問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.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):