Name: SRT 1720 Hydrochloride
Brand: Selleck Chemicals
SKU: S1129
Rating: 5 (190 reviews)

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품질 관리 (Quality Control)

배치: 순도: 99.61%

99.61

함께 자주 사용되는 제품 SRT 1720 Hydrochloride

Selisistat (EX-527)

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

Quercetin (Sophoretin)

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

Astragaloside IV

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

MDL-28170

In combination with MDL-28170, this compound restores the increased level of mitoROS and the reduced membrane potential in human coronary artery endothelial cells (HCAECs), including As-IV.

관련 타겟	HDAC JAK BET Histone Methyltransferase PKC PARP HIF PRMT EZH2 AMPK
기타 Sirtuin 억제제	Sirtinol Fisetin 3-TYP AGK2 SRT2104 (GSK2245840) OSS_128167 SirReal2 SRT2183 Thiomyristoyl Salvianolic acid B

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

세포주	분석 유형	농도	배양 시간	제형	활성 설명	PMID
CACs	Function Assay	4 μM	30 min	DMSO	induces acute SIRT1 activation	26254104
MC3T3-E1	Function Assay	10 µM	1 h		reduces the TGF-β-stimulated VEGF release in dose- and time-dependent manner	26136978
MC3T3-E1	Function Assay	10 µM	12 h		reduces the VEGF mRNA expression levels stimulated by TGF-β	26136978
MC3T3-E1	Function Assay	20 μM	1 h		suppresses the TGF-β-induced phosphorylation of p44/p42 MAP kinase or SAPK/JNK	26136978
WE-68	Apoptosis Assay	0-24 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
SK-N-MC	Apoptosis Assay	0-2.5 μM	24 h		induces cell death in dose dependently	26055805
WE-68	Function Assay	20 μM	0-24 h		activates caspase 3/7	26055805
SK-ES-1	Function Assay	10 μM	0-24 h		activates caspase 3/7	26055805
SK-N-MC	Function Assay	3 μM	0-24 h		activates caspase 3/7	26055805
NRK-49F	Function Assay	0–2 μM	36 h		increases expression of α-SMA and fibronectin dose dependently	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		enhances STAT3 phosphorylation	26022003
RAW264.7	Function Assay	1 μM	6 h		upregulates the reduced SIRT1 protein or mRNA levels by high glucose	25793995
MCF10A	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
T47D	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
MDA-MB-231	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
HS578T	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
A459	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
Neu	Growth Inhibition Assay	0-20 μM	24 h		reduces cell viability dose dependently	25411356
MDA-MB-231	Function Assay	5 μM	8 h		increases the number of acidic vesicular organelles	25411356
MDA-MB-231	Function Assay	5 μM	16 h		induces lysosomal membrane permeabilization	25411356
MC3T3-E1	Function Assay	10 μM	60 min		suppresses the FGF-2-stimulated osteoprotegerin release	25290095
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		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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화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량	506.02	화학식	C₂₅H₂₃N₇OS.HCl	보관 (수령일로부터)	3년-20°C분말
CAS 번호	1001645-58-4	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	N/A			Smiles	C1CN(CCN1)CC2=CSC3=NC(=CN23)C4=CC=CC=C4NC(=O)C5=NC6=CC=CC=C6N=C5.Cl

용해도 (Solubility)

In vitro
배치:

DMSO : 100 mg/mL (197.62 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 100 mg/mL (197.62 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 100 mg/mL (197.62 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 38 mg/mL (75.09 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 45 mg/mL (88.92 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

몰농도 계산기

질량	농도	부피	분자량
=	×	×

희석 계산기 분자량 계산기

In vivo 배치:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	5.000mg/ml (9.88mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

투여량: mg/kg 동물 평균 체중: g 동물당 투여량:μL 동물 수:

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH₂O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘 (Mechanism of Action)

Targets/IC₅₀/Ki	SIRT1 (Cell-free assay) 0.16 μM(EC50)
시험관 내(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. 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. 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.
키나아제 분석	SIRT1 형광 편광 분석
키나아제 분석	SIRT1 FP 분석에서 SIRT1 활성은 p53 서열에서 유래된 20개 아미노산 펩타이드(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)를 사용하여 모니터링됩니다. 이 펩타이드는 N-말단에 비오틴이 연결되어 있고 C-말단은 형광 태그로 변형되어 있습니다. 효소 활성을 모니터링하기 위한 반응은 결합 효소 분석으로, 첫 번째 반응은 SIRT1에 의해 촉매되는 탈아세틸화 반응이며 두 번째 반응은 새로 노출된 리신 잔기에서 트립신에 의한 절단 반응입니다. 반응을 중단시킨 후 스트렙타비딘을 첨가하여 기질과 생성물 사이의 질량 차이를 강조합니다. FP 분석의 민감도를 통해 SRT 1720 Hydrochloride를 식별할 수 있습니다. 형광 편광 반응 조건은 다음과 같습니다: 0.5 μM 펩타이드 기질, 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, 0.15 mM 니코틴아마이드. 반응은 37 °C에서 인큐베이션하고 니코틴아마이드를 첨가하여 중단시키며, 트립신을 첨가하여 탈아세틸화된 기질을 절단합니다. 이 반응은 1 μM 스트렙타비딘 존재 하에 37 °C에서 인큐베이션합니다. 형광 편광은 들뜸(650 nm) 및 방출(680 nm) 파장에서 결정됩니다.
생체 내(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.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/18046409/ [2] https://pubmed.ncbi.nlm.nih.gov/21950728/

적용 분야 (Applications)

방법	바이오마커	PMID
Western blot	Cleaved-PARP-1 / Cleaved-caspase-3 / LC3-II / p62 / SIRT1	26655844
Immunofluorescence	Cathepsin B	26655844
Growth inhibition assay	Cell viability	25411356

자주 묻는 질문 (Frequently Asked Questions)

질문 1:
How can we prepare it for in vivo mouse studies?

답변:
It can be dissolved in 30% PEG 400+0.5% Tween 80+5% Propylene glycol at 30mg/ml as a suspension, which is fine for oral gavage. We’ve also found that it can be dissolved in 2% DMSO+30% PEG 300+1% Tween 80+ddH2O at 3mg/ml clearly, making it suitable for injection. When preparing the solution, please dissolve the compound in DMSO clearly first, then add PEG and Tween. After they are 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):

SRT 1720 Hydrochloride SIRT1 활성제

분자량: 506.02

품질 관리 (Quality Control)

함께 자주 사용되는 제품 SRT 1720 Hydrochloride

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

용해도 (Solubility)

몰농도 계산기

생체 내 제형 계산기 (투명한 용액)

작용 메커니즘 (Mechanism of Action)

적용 분야 (Applications)

자주 묻는 질문 (Frequently Asked Questions)

SRT 1720 Hydrochloride SIRT1 활성제

분자량: 506.02

품질 관리 (Quality Control)

함께 자주 사용되는 제품 SRT 1720 Hydrochloride

세포 배양, 처리 및 작업 농도 (Cell Culture, Treatment & Working Concentration)

화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

용해도 (Solubility)

몰농도 계산기

생체 내 제형 계산기 (투명한 용액)

작용 메커니즘 (Mechanism of Action)

적용 분야 (Applications)

자주 묻는 질문 (Frequently Asked Questions)

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)