GSK-0660 (GSK0660)|supplier DC Chemicals

Cas No.:	1014691-61-2
Chemical Name:	GSK-0660，GSK 0660，GSK0660
Synonyms:	GSK-0660，GSK 0660，GSK0660
SMILES:	COC1=C(C=CC(=C1)NC2=CC=CC=C2)NS(=O)(=O)C3=C(SC=C3)C(=O)OC
Formula:	C₁₉H₁₈N₂O₅S₂
M.Wt:	418.49
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

GSK0660 is a potent antagonist of PPARβ and PPARδ, with IC50s of 155 nM for both isoforms.

In Vitro:

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[1]. GSK0660 (0.5 μM) reduces the levels of AMPK and eNOS phosphorylation, and BMP-2, Runx-2 mRNA expression in MC3T3-E1 cells. GSK0660 (0.1 and 0.5 μM) reverses the bezafibrate-induced enchancement of ALP activity on d 7 in MC3T3-E1 cells[2]. 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. Furthermore, GSK0660 significantly reduces inhibitory effect of GW501516 on the LPS-induced expression of gp91phox mRNA in BV-2 cells[3].

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101

Cat. No.	Product name	Field of application
DC9602	Balaglitazone	Balaglitazone (DRF-2593; NN-2344) is a novel partial agonist of PPAR-γ.
DC7412	R(+)-Etomoxir (sodium salt)	A PPARα agonist and an irreversible CPT-1 inhibitor.
DC1034	WY14643 (Pirinixic Acid)	WY 14643 (Pirinixic Acid) is a potent peroxisome proliferator and activator of PPARα with ED50 of 1.5 μM.
DC10700	Seladelpar	Seladelpar is a selective peroxisome proliferator-activated receptor (SPPAR) -δ receptor agonist.
DC12034	MA-0204	MA-0204 is a potent, selective PPARδ modulator with good pharmacokinetic properties.
DC2079	GW-9662	GW9662 is a selective PPAR antagonist, inhibiting PPARγ, PPARα and PPARδ with IC50 of 3.3 nM, 32 nM and 2 μM, respectively.
DC4233	GW501516	GW501516 is the most selective and potent PPARβ (EC50=1.1nM) agonist that has been demonstrated to be 1,000-fold more selective in comparison to existing subtypes.
DC9904	GW0742	GW0742 is a potent PPARβ and PPARδ agonist, with an IC50 of 1 nM for human PPARδ in binding assay, and EC50s of 1 nM, 1.1 μM and 2 μM for human PPARδ, PPARα, and PPARγ, respectively.
DC2078	GW-7647	GW 7647 is a potent PPARα agonist with 200-fold selectivity over PPARγ and PPARδ.
DC1035	GSK3787	GSK3787 is as a potent and selective antagonist of PPARδ with pIC50 of 6.6.