Home Metabolism PPAR agonist GW501516 For research use only.

GW501516

Synonyms: GW 1516 ,GSK-516

GW501516 is a potent and highly selective PPARβ/δ agonist, with EC50 of 1 nM, with 1000-fold selectivity over hPPARα and hPPARγ. Phase 4.

GW501516 Chemical Structure

GW501516 Chemical Structure

CAS No. 317318-70-0

Purity & Quality Control

GW501516 Related Products

Signaling Pathway

PPAR Signaling Pathways

PPAR Signaling Pathway

Biological Activity

Description GW501516 is a potent and highly selective PPARβ/δ agonist, with EC50 of 1 nM, with 1000-fold selectivity over hPPARα and hPPARγ. Phase 4.
Features A selective PPARδ agonist compared with a synthetic LXRα agonist GW3965.
Targets
PPARδ [1]
1.1 nM(EC50)
In vitro
In vitro GW501516 is demonstrated to be 1000-fold more selective in comparison to existing subtypes. GW501516 increases expression of the reverse cholesterol transporter ATP-binding cassette A1 and induces apolipoprotein A1-specific cholesterol efflux In macrophages, fibroblasts, and intestinal cells. [2] GW501516 can regulate expression of genes involved in lipid catabolism and energy uncoupling in skeletal muscle cells. [4] Additionally, GW501516 is shown to block insulin resistance and fatty acid-induced nuclear factor-κB activation. [5] GW 501516 reduces the IFNγ-induced up-regulation of TNFα and inducible NO synthase, and showed anti-inflammatory activity. [6]
In Vivo
In vivo GW501516 dramatically increases serum high density lipoprotein cholesterol while lowering the levels of small-dense low density lipoprotein, fasting triglycerides, and fasting insulin when dosed to insulin-resistant middle-aged obese rhesus monkeys. [2] GW501516 induces fatty acid β-oxidation in L6 myotubes and in mouse skeletal muscles. GW501516 treatment to mice fed a high-fat diet ameliorates diet-induced obesity as well as insulin resistance. GW501516 treatment also dramatically improves diabetes, as demonstrated by the decrease in plasma glucose and blood insulin levels in genetically obese ob/ob mice. [7]
Animal Research Animal Models Male obese rhesus monkey
Dosages 0.1, 0.3, 1.0, and 3.0 mg/kg
Administration Orally

Chemical Information & Solubility

Molecular Weight 453.50 Formula

C21H18F3NO3S2
CAS No. 317318-70-0 SDF Download GW501516 SDF
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 91 mg/mL ( (200.66 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 22 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

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.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy GW501516 | GW501516 supplier | purchase GW501516 | GW501516 cost | GW501516 manufacturer | order GW501516 | GW501516 distributor