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

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Control de calidad (Quality Control)

Lote: Pureza: 99.61%

99.61

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Dianas relacionadas	HDAC JAK BET Histone Methyltransferase PKC PARP HIF PRMT EZH2 AMPK
Otros Sirtuin Inhibidores	Sirtinol Fisetin 3-TYP AGK2 SRT2104 (GSK2245840) OSS_128167 SirReal2 SRT2183 Thiomyristoyl Salvianolic acid B

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)

Líneas celulares	Tipo de ensayo	Concentración	Tiempo de incubación	Formulación	Descripción de la actividad	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
Haga clic para ver más datos experimentales de líneas celulares

Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular	506.02	Fórmula	C₂₅H₂₃N₇OS.HCl	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	1001645-58-4	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	N/A			Smiles	C1CN(CCN1)CC2=CSC3=NC(=CN23)C4=CC=CC=C4NC(=O)C5=NC6=CC=CC=C6N=C5.Cl

Solubilidad (Solubility)

In vitro
Lote:

DMSO : 100 mg/mL (197.62 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Water : Insoluble

Ethanol : Insoluble

Calculadora de Molaridad

Masa	Concentración	Volumen	Peso molecular
=	×	×

Calculadora de Dilución Calculadora de Peso Molecular

In vivo Lote:
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 Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	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.

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

Dosis: mg/kg Peso promedio de los animales: g Volumen de dosificación por animal:μL Número de animales:

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH₂O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción (Mechanism of Action)

Targets/IC₅₀/Ki	SIRT1 (Cell-free assay) 0.16 μM(EC50)
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.
Ensayo de quinasa	Ensayo de polarización de fluorescencia SIRT1
Ensayo de quinasa	En el ensayo FP de SIRT1, la actividad de SIRT1 se monitoriza utilizando un péptido de 20 aminoácidos (Ac-Glu-Glu-Lys(biotin)-Gly-Gln-Ser-Thr-Ser-Ser-His-Ser-Lys(Ac)-Nle-Ser-Thr-Glu-Gly–Lys(MR121 o Tamra)-Glu-Glu-NH₂) derivado de la secuencia de p53. El péptido está unido N-terminalmente a biotina y modificado C-terminalmente con una etiqueta fluorescente. La reacción para monitorizar la actividad enzimática es un ensayo enzimático acoplado donde la primera reacción es la reacción de desacetilación catalizada por SIRT1 y la segunda reacción es la escisión por tripsina en el residuo de lisina recién expuesto. La reacción se detiene y se añade estreptavidina para acentuar las diferencias de masa entre el sustrato y el producto. La sensibilidad del ensayo FP permite la identificación de SRT1720. Las condiciones de la reacción de polarización de fluorescencia son las siguientes: 0,5 μM de sustrato peptídico, 150 μM de βNAD⁺, 0-10 nM de SIRT1, 25 mM de Tris-acetato pH 8, 137 mM de Na-Ac, 2,7 mM de K-Ac, 1 mM de Mg-Ac, 0,05 % de Tween-20, 0,1 % de Pluronic F127, 10 mM de CaCl 2, 5 mM de DTT, 0,025 % de BSA y 0,15 mM de nicotinamida. La reacción se incuba a 37 °C y se detiene añadiendo nicotinamida, y se añade tripsina para escindir el sustrato desacetilado. Esta reacción se incuba a 37 °C en presencia de 1 μM de estreptavidina. La polarización fluorescente se determina a longitudes de onda de excitación (650 nm) y emisión (680 nm).
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.
Referencias	[1] https://pubmed.ncbi.nlm.nih.gov/18046409/ [2] https://pubmed.ncbi.nlm.nih.gov/21950728/

Aplicaciones (Applications)

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

Preguntas frecuentes (Frequently Asked Questions)

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

Respuesta:
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 Activador de SIRT1

Peso molecular: 506.02

Control de calidad (Quality Control)

Productos que se suelen utilizar junto con SRT 1720 Hydrochloride

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)

Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Solubilidad (Solubility)

Calculadora de Molaridad

Calculadora de formulación in vivo (Solución clara)

Mecanismo de acción (Mechanism of Action)

Aplicaciones (Applications)

Preguntas frecuentes (Frequently Asked Questions)

SRT 1720 Hydrochloride Activador de SIRT1

Peso molecular: 506.02

Control de calidad (Quality Control)

Productos que se suelen utilizar junto con SRT 1720 Hydrochloride

Cultivo celular, tratamiento y concentración de trabajo (Cell Culture, Treatment & Working Concentration)

Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Solubilidad (Solubility)

Calculadora de Molaridad

Calculadora de formulación in vivo (Solución clara)

Mecanismo de acción (Mechanism of Action)

Aplicaciones (Applications)

Preguntas frecuentes (Frequently Asked Questions)

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)