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SR-18292

产品编号 T4353 CAS 2095432-55-4

别名: SR 18292

SR-18292 是一种 PPARγ 共激活因子-1α (PGC-1α) 抑制剂，可增加 PGC-1α 乙酰化，抑制糖异生基因表达并减少肝细胞中的葡萄糖生成。

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SR-18292, CAS 2095432-55-4

规格	价格/CNY	货期
1 mg	￥ 235	现货
2 mg	￥ 333	现货
5 mg	￥ 543	现货
10 mg	￥ 796	现货
25 mg	￥ 1,490	现货
50 mg	￥ 2,620	现货
100 mg	￥ 4,390	现货
500 mg	￥ 9,480	现货
1 mL * 10 mM (in DMSO)	￥ 642	现货

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纯度: 99.27%

纯度: 99%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	SR-18292 is an inhibitor of PPAR gamma coactivator-1α (PGC-1α), which increases PGC-1α acetylation, suppresses gluconeogenic gene expression and reduces glucose production in hepatocytes.
靶点活性	PGC1α:NA
体外活性	The transcriptional coactivator PGC-1α plays a pivotal role in energy homeostasis by co-activating transcription factors that regulate fat and glucose metabolism. SR-18292 increases the interaction of PGC-1α with the acetyl transferase GCN5 and reduces co-activation of nuclear hormone receptor HNF4α by PGC-1α. SR-18292 suppresses HNF4α/PGC-1α gluconeogenic transcriptional function. SR-18292 increases the acetylation of specific PGC-1α lysine residues by increasing the interaction of GCN5 with PGC-1α, which might subsequently decrease its gluconeogenic activity.
体内活性	SR-18292 reduces fasting blood glucose, increases hepatic insulin sensitivity and improves glucose homeostasis in diabetic mice. The high fat diet (HFD) fed mice, a dietary model of obesity and T2D, are treated with SR-18292 (45 mg/kg) via I.P. injection for 3 consecutive days and again on day 4 before measuring fasting blood glucose. Strikingly, mice that are treated with SR-18292 have significantly lower levels of fasting blood glucose concentrations than matched vehicle-treated control mice. The induction of gluconeogenic gene expression is a regulatory component of the response to fasting. It is important that gluconeogenic gene expression, specifically that of Pck1, is inhibited in livers isolated from mice treated with SR-18292.
激酶实验	For determination of GCN5 HAT activity U-2 OS cells overexpressing Ad-GCN5 are treated with SR-18292 (10 μM) for 18 h. Cells are lysed with buffer B (20 mM HEPES-KOH (pH 7.9), 125 mM NaCl, 1 mM EDTA, 1 mM DTT, 1% IGEPAL (v/v), 10% glycerol (v/v), 5 mM NaF, 5 mM β-glycerophosphate, 5 mM sodium butyrate and 10 mM nicotinamide), supplemented with Protease Inhibitor Cocktail. FLAG-GCN5 is immunoprecipitated with FLAG beads overnight at 4°C following multiple washes with lysis buffer. GCN5 is then eluted using 3× FLAG peptide and the purified protein is used to determine HAT activity using the HAT Inhibitor Screening Assay Kit
细胞实验	For cell viability determination using MTT, primary hepatocytes are seeded on a 96-well plate at 20,000 cells/well. The following day cells are treated at different doses, as indicated, for 18 h treatment of primary hepatocytes. 5 μL of MTT reagent (5 mg/mL) is then added to each well (n=4/dose) and cells are incubated for 1h at 37°C. Medium is discarded and dye is extracted by adding 100 μL DMSO to each well. For cytotoxicity determination using ToxiLight Non-destructive Cytotoxicity Bioassay, hepatocytes are seeded on a 6-well plate and treated with either SR-18292 (20 μM) or Cisplatin (50 μM) for 18 h. 50 μL of medium is collected and used to measure cellular toxicity by adding 100 of adenylate kinase detection reagent and incubating 5 min at RT before measuring luminescence[
动物实验	SR-18292 is re-suspended in a 10% DMSO/10% Tween80/80% PBS solution at a final concentration of 6-12 mg/mL.MiceFor in vivo studies with DIO mice, males 6-8 weeks old are fed high fat diet (HFD) for the indicated time. For drug administration, SR-18292 (45 mg/kg) is injected via I.P. for 3 days between 4-5 pm and food is removed on day 3 at 5pm. The following morning (day 4) SR-18292 is injected again (for a total of 4 injections) and blood glucose is measured after 3 hours. Injection volume does not exceed 275 μL per mouse

别名	SR 18292
分子量	366.5
分子式	C23H30N2O2
CAS No.	2095432-55-4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 10 mg/mL

DMSO: 55 mg/mL (150.06 mM)

H2O: Insoluble

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7285 mL	13.6426 mL	27.2851 mL	68.2128 mL
	5 mM	0.5457 mL	2.7285 mL	5.457 mL	13.6426 mL
	10 mM	0.2729 mL	1.3643 mL	2.7285 mL	6.8213 mL
	20 mM	0.1364 mL	0.6821 mL	1.3643 mL	3.4106 mL
	50 mM	0.0546 mL	0.2729 mL	0.5457 mL	1.3643 mL
	100 mM	0.0273 mL	0.1364 mL	0.2729 mL	0.6821 mL

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摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

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配液浓度

参考文献

1. Sharabi K,etal.Selective Chemical Inhibition of PGC-1α Gluconeogenic Activity Ameliorates Type 2 Diabetes.Cell. 2017 Mar 23;169(1):148-160.

文献引用

1. Wang L, Xie Y, Xiao B, et al.Isorhamnetin alleviates cisplatin-induced acute kidney injury via enhancing fatty acid oxidation.Free Radical Biology and Medicine.2023

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

SR-18292 2095432-55-4 Autophagy Metabolism SR18292 PPARγ coactivator-1α PGC-1α SR 18292 Inhibitor inhibit inhibitor

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SR-18292

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参考文献

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剂量换算

体内实验配液计算器

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