Home Tools
Log in
Cart

SR-18292

Catalog No. T4353   CAS 2095432-55-4
Synonyms: SR 18292

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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
SR-18292 Chemical Structure
SR-18292, CAS 2095432-55-4
Pack Size Availability Price/USD Quantity
2 mg In stock $ 34.00
5 mg In stock $ 55.00
10 mg In stock $ 89.00
25 mg In stock $ 189.00
50 mg In stock $ 297.00
100 mg In stock $ 472.00
500 mg In stock $ 987.00
1 mL * 10 mM (in DMSO) In stock $ 65.00
Bulk Inquiry
Get quote
Select Batch  
Purity: 99.36%
Purity: 99.27%
Purity: 99%
Contact us for more batch information
Biological Description
Chemical Properties
Storage & Solubility Information
Description 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.
Targets&IC50 PGC-1α:NA
In vitro 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.
In vivo 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.
Kinase Assay 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
Cell Research 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[
Animal Research 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
Synonyms SR 18292
Molecular Weight 366.5
Formula C23H30N2O2
CAS No. 2095432-55-4

Storage

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

Solubility Information

Ethanol: 10 mg/mL

DMSO: 55 mg/mL (150.06 mM)

H2O: Insoluble

TargetMolReferences and Literature

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

TargetMolCitations

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

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compounds Library Max Anti-Metabolism Disease Compound Library NO PAINS Compound Library Glycometabolism Compound Library Autophagy Compound Library Anti-Diabetic Compound Library Anti-COVID-19 Compound Library Lipid Metabolism Compound Library Anti-Obesity Compound Library Stem Cell Differentiation Compound Library

Related Products

Related compounds with same targets
SBI-0640756 3PO Mycro 3 Rutin hydrate Ambroxol hydrochloride Zoledronic acid monohydrate Clemastine fumarate CX546

TargetMolDose Conversion

You can also refer to dose conversion for different animals. More

TargetMol In vivo Formulation Calculator (Clear solution)

Step One: Enter information below
Dosage
mg/kg
Average weight of animals
g
Dosing volume per animal
ul
Number of animals
Step Two: Enter the in vivo formulation
% DMSO
%
% Tween 80
% ddH2O
Calculate Reset

TargetMolCalculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculation
Molecular Weight Calculator
=
X
X

Molarity Calculator allows you to calculate the

  • Mass of a compound required to prepare a solution of known volume and concentration
  • Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Concentration of a solution resulting from a known mass of compound in a specific volume
See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

X
=
X

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

=
/

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

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

 

TargetMol