Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
1 mg
5 mg
10 mg
1 mM
2.3895 mL
11.9477 mL
23.8954 mL
5 mM
0.4779 mL
2.3895 mL
4.7791 mL
10 mM
0.2390 mL
1.1948 mL
2.3895 mL
50 mM
0.0478 mL
0.2390 mL
0.4779 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.
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.