Name: SR-18292
Brand: Selleck Chemicals
SKU: S8528
Rating: 5 (4 reviews)

SR-18292 inhibits PGC-1α gluconeogenic activity and reduces co-activation of HNF4α by modulating the interaction between GCN5 and PGC-1α.

SR-18292 Chemical Structure

CAS: 2095432-55-4

Selleck's SR-18292 has been cited by 4 publications

Purity & Quality Control

Batch: Purity: 99.16%

99.16

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Biological Activity

Description

SR-18292 inhibits PGC-1α gluconeogenic activity and reduces co-activation of HNF4α by modulating the interaction between GCN5 and PGC-1α.

Targets

PGC-1α ^[1]

In vitro
In vitro	SR-18292 is a potent inhibitor of the gluconeogenic gene expression and glucose production in hepatocytes. It increases the interaction of PGC-1α with GCN5 and reduces co-activation of HNF4α by PGC-1α. SR-18292 suppresses HNF4α/PGC-1α gluconeogenic transcriptional function^[2].
Cell Research	Cell lines	U-2 OS cells overexpressing Ad-GCN5
	Concentrations	10 μM
	Incubation Time	18 h
	Method	For determination of GCN5 HAT activity U-2 OS cells overexpressing Ad-GCN5 are treated with SR-18292 (10μM) 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℃ 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.
Experimental Result Images	Methods	Biomarkers	Images	PMID
Experimental Result Images	Western blot	PGC1-α / GCN5		28340340

In Vivo
In vivo	SR-18292 reduces blood glucose, strongly increases hepatic insulin sensitivity and improves glucose homeostasis in dietary and genetic mouse models of type 2 diabetes. SR-18292 suppresses hepatic glucose production and increases liver insulin sensitivity in vivo. The liver is a major target of SR-18292 and probably accounts for a significant part of its anti-diabetic effects^[1].
Animal Research	Animal Models	a high fat diet (HFD) fed mice, a dietary model of obesity and type 2 diabates
	Dosages	45 mg/kg
	Administration	i.p.

References

[1] Sharabi K, et al. Cell. 2017, 169(1):148-160.

Chemical Information & Solubility

Molecular Weight	366.50	Formula	C₂₃ H₃₀ N₂O₂
CAS No.	2095432-55-4	SDF	--
Smiles	CC1=CC=C(C=C1)CN(CC(COC2=CC=CC3=C2C=CN3)O)C(C)(C)C
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 73 mg/mL ( (199.18 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 73 mg/mL

Water : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.					In vivo Formulation Calculator
	Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.1mg/ml (13.92mM)	Taking the 1 mL working solution as an example, add 50 μL of 102 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 clarify; 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.	In vivo Formulation Calculator
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.0mg/ml (13.64mM)
	5% DMSO 1 95% Corn oil	0.312mg/ml (0.85mM)

Preparing Stock Solutions

Molarity Calculator

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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