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GSK0660
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GSK0660图片
CAS NO:1014691-61-2
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 418.49
Formula C19H18N2O5S2
CAS No.1014691-61-2
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: ≥ 49 mg/mL
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo) O=C(C1=C(S(=O)(NC2=CC=C(NC3=CC=CC=C3)C=C2OC)=O)C=CS1)OC
Synonyms GSK0660; GSK-0660; GSK 0660
实验参考方法
In Vitro

In vitro activity: GSK0660 is a potent antagonist of PPARβ and PPARδ, with IC50s of both 155 nM, and is nearly inactive on PPARα and PPARγ with IC50s of both>10 μM.GSK0660 (100 nM) reduces CPT1a (a PPARβ/δ target gene) expression below the basal vehicle-treated level by approximately 50%, but shows no effect on PDK4 expression, which is also a PPARβ/δ target gene in skeletal muscle cells.GSK0660 (1 μM) markedly blocks GW501516-mediated attenuation of glutamate release, and the effect of GW501516 on ROS generation in BV-2 cells stimulated with LPS.GSK0660 (0.5 μM) reduces the levels of AMPK and eNOS phosphorylation, and BMP-2, Runx-2 mRNA expression in MC3T3-E1 cells.


Kinase Assay: GSK0660 is a potent antagonist of PPARβ and PPARδ, with IC50s of both 155 nM, and is nearly inactive on PPARα and PPARγ with IC50s of both>10 μM. GSK0660 antagonizes 100% of the activity of PPARβ/δ with a pIC50 of 6.8. GSK0660 (100 nM) reduces CPT1a (a PPARβ/δ target gene) expression below the basal vehicle-treated level by approximately 50%, but shows no effect on PDK4 expression, which is also a PPARβ/δ target gene in skeletal muscle cells.


Cell Assay: GSK0660 is dissolved in DMSO.Cell viability is determined by the MTT dye. MC3T3-E1 cells are incubated with bezafibrate (1–1000 μM) for 24, 48, or 72 h, and are pretreated with the AMPK inhibitor compound C (5 μM), PPARβ inhibitor GSK0660 (0.5 μM), PPARα inhibitor MK886 (10 μM), or NOS inhibitor L-NAME (1000 μM) followed by bezafibrate (100 μM) incubation for 48 h. After the incubations, 10 μL of MTT is added to each well of a 96-well microplate, and the microplates are placed in an incubator at 37°C for 4 h.

In Vivo
Animal model
Formulation & Dosage
References Mol Endocrinol. 2008 Feb;22(2):523-9. Epub 2007 Nov 1.Acta Pharmacol Sin. 2011 May;32(5):591-600.J Cell Biochem. 2018 Feb 1.