|SRT1720 盐酸盐|CsnPharm

CAS No.: 2060259-60-9

盐酸盐 Catalog No. CSN15828

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%.

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400-920-2911

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tech@csnpharm.cn

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400-920-2911

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Sirtuin 1

EC1.5:0.16μM Sirtuin 2

EC1.5:37μM Sirtuin 3

EC1.5:300μM
描述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. 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.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
9607	1 μM	Cell Viability Assay	36 h	increases the cell viability compared with melatonin alone	23726949
9607	1 μM	Function Assay	36 h	increases SIRT1 and decreased acetylated-p53 expression	23726949
A459	0-20 μM	Growth Inhibition Assay	24 h	reduces cell viability dose dependently	25411356

动物研究

剂量

Rat: 5 mg/kg^[3] (i.p.) Mice: 10 mg/kg - 100 mg/kg^[2] (p.o.); Nude Mice: 50 mg/kg - 200 mg/kg^[4] (p.o.)

给药途径

p.o.

动物药代数据

Animal	Mice^[2]
Dose	100 mg/kg
Administration	p.o.
F	0.5
T_1/2	~ 5 h
AUC	7892 ng/h/ml

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9762 mL
- 9.8810 mL
- 19.7620 mL
- 5 mM
- 0.3952 mL
- 1.9762 mL
- 3.9524 mL
- 10 mM
- 0.1976 mL
- 0.9881 mL
- 1.9762 mL

技术信息

CAS号

2060259-60-9

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H24ClN7OS

运输

蓝冰

分子量

506.02

别名

溶解度

DMSO	11.0 mg/mL (21.7 mM)
Water	7.33 mg/mL (14.5 mM)

动物实验配方

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

9607	1 μM	Cell Viability Assay	36 h	increases the cell viability compared with melatonin alone	23726949
9607	1 μM	Function Assay	36 h	increases SIRT1 and decreased acetylated-p53 expression	23726949
A459	0-20 μM	Growth Inhibition Assay	24 h	reduces cell viability dose dependently	25411356
BT20	0-20 μM	Growth Inhibition Assay	24 h	reduces cell viability dose dependently	25411356
CACs	4 μM	Function Assay	30 min	induces acute SIRT1 activation	26254104
H411EC3	50/100 nM	Function Assay	6 h	increases SIRT1 activity in the presence of TSA, PEPCK activity, mRNA levels of Pck1 and Pgc1α, and elevating glucose production	21212096
HCT116	0-20 μM	Growth Inhibition Assay	24 h	reduces cell viability dose dependently	25411356
hepatocytes	10 nM	Function Assay	6 h	increases SIRT1 activity in the presence of TSA, PEPCK activity, mRNA levels of Pck1 and Pgc1α, and elevating glucose production	21212096
hepatocytes	10 nM	Function Assay	6 h	increases Hmgcr and Acc gene expression	21212096
HS578T	0-20 μM	Growth Inhibition Assay	24 h	reduces cell viability dose dependently	25411356
Ina6	7/10 μM	Cell Viability Assay	24 h	decreases viability concentration dependently	21950728
KMS12	7/10 μM	Cell Viability Assay	24 h	decreases viability concentration dependently	21950728
LR5	7/10 μM	Cell Viability Assay	24 h	decreases viability concentration dependently	21950728
MC3T3-E1	10 µM	Function Assay	1 h	reduces the TGF-β-stimulated VEGF release in dose- and time-dependent manner	26136978
MC3T3-E1	10 µM	Function Assay	12 h	reduces the VEGF mRNA expression levels stimulated by TGF-β	26136978
MC3T3-E1	20 μM	Function Assay	1 h	suppresses the TGF-β-induced phosphorylation of p44/p42 MAP kinase or SAPK/JNK	26136978
MC3T3-E1	10 μM	Function Assay	60 min	suppresses the FGF-2-stimulated osteoprotegerin release	25290095
MC3T3-E1	10 μM	Function Assay	60 min	attenuates the FGF-2-induced osteoprotegerin mRNA expression	25290095
MC3T3-E1	10 μM	Function Assay	60 min	attenuates the FGF-2-induced osteoprotegerin mRNA expression	25290095
MC3T3-E1	10 μM	Function Assay	60 min	suppresses the BMP-4-stimulated VEGF release	24435444
MC3T3-E1	10 μM	Function Assay	60 min	suppresses the PGF2α-stimulated OPG release	24333336
MC3T3-E1	10 μM	Function Assay	60 min	reduces the PGF2α-stimulated phosphorylation of p44/p42 MAP kinase	24333336
MC3T3-E1	10 μM	Function Assay	60 min	attenuates the PGF2α-induced phosphorylation of both MEK1/2 and Raf-1	24333336
MCF10A	0-20 μM	Growth Inhibition Assay	24 h	reduces cell viability dose dependently	25411356
MCF-7	0-20 μM	Growth Inhibition Assay	24 h	reduces cell viability dose dependently	25411356
MDA-MB-231	0-20 μM	Growth Inhibition Assay	24 h	reduces cell viability dose dependently	25411356
MDA-MB-231	5 μM	Function Assay	8 h	increases the number of acidic vesicular organelles	25411356
MDA-MB-231	5 μM	Function Assay	16 h	induces lysosomal membrane permeabilization	25411356
MM.1R	7/10 μM	Cell Viability Assay	24 h	decreases viability concentration dependently	21950728
MM.1R	7/10 μM	Apoptosis Assay	24 h	induces a significant increase in the Annexin V+/PI− apoptosis	21950728
MM.1S	7/10 μM	Cell Viability Assay	24 h	decreases viability concentration dependently	21950728
Neu	0-20 μM	Growth Inhibition Assay	24 h	reduces cell viability dose dependently	25411356
NRK-49F	0–2 μM	Function Assay	36 h	increases expression of α-SMA and fibronectin dose dependently	26022003
NRK-49F	0–2 μM	Function Assay	36 h	enhances phosphorylation of EGFR and PDGFRβ	26022003
NRK-49F	0–2 μM	Function Assay	36 h	enhances STAT3 phosphorylation	26022003
RAW264.7	1 μM	Function Assay	6 h	upregulates the reduced SIRT1 protein or mRNA levels by high glucose	25793995
RPE	5 µM	Cell Viability Assay	1 h	attenuates OAβ-induced decrease of cell viability	24036938
RPMI.8226	7/10 μM	Cell Viability Assay	24 h	decreases viability concentration dependently	21950728
RPMI-8226	7/10 μM	Apoptosis Assay	24 h	induces a significant increase in the Annexin V+/PI− apoptosis	21950728
SKBR3	0-20 μM	Growth Inhibition Assay	24 h	reduces cell viability dose dependently	25411356
SK-ES-1	0-10 μM	Apoptosis Assay	24 h	induces cell death in dose dependently	26055805
SK-ES-1	10 μM	Function Assay	0-24 h	activates caspase 3/7	26055805
SK-N-MC	0-2.5 μM	Apoptosis Assay	24 h	induces cell death in dose dependently	26055805
SK-N-MC	3 μM	Function Assay	0-24 h	activates caspase 3/7	26055805
SUM149	0-20 μM	Growth Inhibition Assay	24 h	reduces cell viability dose dependently	25411356
T47D	0-20 μM	Growth Inhibition Assay	24 h	reduces cell viability dose dependently	25411356
U266	7/10 μM	Cell Viability Assay	24 h	decreases viability concentration dependently	21950728
WE-68	0-24 μM	Apoptosis Assay	24 h	induces cell death in dose dependently	26055805
WE-68	20 μM	Function Assay	0-24 h	activates caspase 3/7	26055805

靶点	Description	IC50
Sirtuin 1		EC1.5:0.16μM
Sirtuin 2		EC1.5:37μM
Sirtuin 3		EC1.5:300μM

盐酸盐 Catalog No. CSN15828

靶点选择性

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