Home Metabolism PPAR antagonist GSK0660 For research use only.

GSK0660

GSK0660 is a potent PPARβ/δ antagonist with a pIC50 of 6.8 (binding assay IC50 = 155 nM; antagonist assay IC50 = 300 nM) and is nearly inactive on PPARα and PPARγ with IC50s above approximately 10 μM.

GSK0660 Chemical Structure

GSK0660 Chemical Structure

CAS: 1014691-61-2

Selleck's GSK0660 has been cited by 3 publications

Purity & Quality Control

Batch: S581701 DMSO] 84 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.75%
99.75

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Signaling Pathway

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Biological Activity

Description GSK0660 is a potent PPARβ/δ antagonist with a pIC50 of 6.8 (binding assay IC50 = 155 nM; antagonist assay IC50 = 300 nM) and is nearly inactive on PPARα and PPARγ with IC50s above approximately 10 μM.
Targets
PPAR-β/δ [1]
(binding assay)
155 nM
In vitro
In vitro GSK0660 inhibits HRMEC (human retinal microvascular endothelial cells) proliferation and differentiation[2].
Cell Research Cell lines HRMECs
Concentrations 0.01, 0.1, or 1.0 μM
Incubation Time 6 h
Method

HRMECs were seeded in six-well plates at 2 × 105 cells/well and maintained under standard tissue culture conditions. At 80% confluency, the cells were serum starved for 12 hours, then treated on a background of 0.5% serum-containing vehicle (0.1% DMSO) or PPAR-β/δ agonist GW0742 (0.01, 0.1, or 1.0 μM) or on a background of 2% serum-containing vehicle or PPAR-β/δ antagonist GSK0660 (0.01, 0.1, or 1.0 μM) for 6 hours. Cells were washed twice with cold PBS and total RNA was collected. Total RNA isolated from the culture wells was reverse transcribed. Quantitative RT-PCR was performed.
In Vivo
In vivo GSK0660 is rapidly cleared and does not accumulate in the blood in vivo[1]. GSK0660 is efficacious against retinal NV when administered by IVIT or IP injection. Intravitreal injection has the advantages of producing high levels of drug at active sites of neovascular disease, but deleterious side effects are associated with this route of drug administration, including endophthalmitis, cataractogenesis, and glaucoma. Systemic administration could avoid these side effects, but it is hampered by the need for repeated dosing to obtain target concentrations of active drug in diseased tissues. It also needlessly exposes disease-free organs and tissues to active drug[2].
Animal Research Animal Models Sprague-Dawley rat
Dosages 0.2 or 1.0 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 418.49 Formula

C19H18N2O5S2
CAS No. 1014691-61-2 SDF --
Smiles COC1=C(C=CC(=C1)NC2=CC=CC=C2)NS(=O)(=O)C3=C(SC=C3)C(=O)OC
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 84 mg/mL ( (200.72 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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. )

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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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