[CAS NO. 1014691-61-2]  GSK0660

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PRODUCTS SPECIFICATIONS [1014691-61-2]

Store
Catalog
SLK-S5817
Brand
Selleck
CAS
1014691-61-2

DESCRIPTION [1014691-61-2]

Overview

MDLMFCD12828770
Molecular Weight418.49
Molecular FormulaC19H18N2O5S2
SMILESO=C(C1=C(S(=O)(NC2=CC=C(NC3=CC=CC=C3)C=C2OC)=O)C=CS1)OC

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM2.3895 mL11.9477 mL23.8954 mL
5 mM0.4779 mL2.3895 mL4.7791 mL
10 mM0.2390 mL1.1948 mL2.3895 mL
50 mM0.0478 mL0.2390 mL0.4779 mL

Description

GSK0660 is a potent 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

GSK0660 inhibits HRMEC (human retinal microvascular endothelial cells) proliferation and differentiation.

In vivo

GSK0660 is rapidly cleared and does not accumulate in the blood in vivo. 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.