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SR-18292 PGC-1α inhibitor

Name: SR-18292
Brand: Selleck Chemicals
SKU: S8528
Availability: InStock
Rating: 5 (6 reviews)

Cat.No.S8528

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

Chemical Structure

Molecular Weight: 366.50

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability

Quality Control

Batch: Purity: 99.16%

99.16

Related Targets	P450 (e.g. CYP17) Dehydrogenase PDE phosphatase PPAR HSP Vitamin Transferase Carbohydrate Metabolism Mitochondrial Metabolism Drug Metabolite Casein Kinase Serine/threonin kinase Lipoxygenase LPL Receptor Phospholipase (e.g. PLA) Retinoid Receptor DPP ACE Peroxidases Amino Acids and Derivatives Fatty Acid Synthase Glucokinase FXR HMG-CoA Reductase Carbonic Anhydrase Lipase Decarboxylase DHFR IDO/TDO
Related Products	ZLN005 PGC-1α Antibody [J17F10] PGC1α/β Antibody [H5N22] Gynostemma pentaphyllum Extract

Chemical Information, Storage & Stability

Molecular Weight	366.50	Formula	C₂₃ H₃₀ N₂O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	2095432-55-4	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=CC=C(C=C1)CN(CC(COC2=CC=CC3=C2C=CN3)O)C(C)(C)C

Solubility

In vitro
Batch:

DMSO : 73 mg/mL (199.18 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 73 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
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 Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.100mg/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.
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.
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (13.64mM)
	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.312mg/ml (0.85mM)

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

% DMSO

Calculation results:

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.

Mechanism of Action

Targets/IC₅₀/Ki	PGC-1α ^[1]
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. This compound suppresses HNF4α/PGC-1α gluconeogenic transcriptional function^[2].
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. This compound suppresses hepatic glucose production and increases liver insulin sensitivity in vivo. The liver is a major target of this chemical and probably accounts for a significant part of its anti-diabetic effects^[1].
References	[1] https://pubmed.ncbi.nlm.nih.gov/28340340/

Applications

Methods	Biomarkers	Images	PMID
Western blot	PGC1-α / GCN5		28340340

Tech Support

Handling Instructions

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