DC Chemicals Limited
China
Product Name: GSK-0660
Price: $400.0/100mg $800.0/250mg $1600.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: 3-[[[2-Methoxy-4-(phenylamino)phenyl]amino]sulfonyl]-2-thiophenecarboxylicacidmethylester
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

1014691-61-2

1014691-61-2 structure

1014691-61-2 structure

Name: GSK0660
Chemical Name: methyl 3-[(4-anilino-2-methoxyphenyl)sulfamoyl]thiophene-2-carboxylate
CAS Number: 1014691-61-2
Molecular Formula: C₁₉H₁₈N₂O₅S₂
Molecular Weight: 418.487
Catalog: Research Areas Metabolic Disease
Create Date: 2016-05-23 10:59:28
Modify Date: 2024-01-14 18:24:23
GSK0660 is a potent antagonist of PPARβ and PPARδ, with IC50s of 155 nM for both isoforms.

Name	methyl 3-[(4-anilino-2-methoxyphenyl)sulfamoyl]thiophene-2-carboxylate
Synonyms	Methyl 3-[(4-anilino-2-methoxyphenyl)sulfamoyl]-2-thiophenecarboxylate 2-Thiophenecarboxylic acid, 3-[[[2-methoxy-4-(phenylamino)phenyl]amino]sulfonyl]-, methyl ester gsk0660 Methyl 3-[(4-anilino-2-methoxyphenyl)sulfamoyl]thiophene-2-carboxylate qcr-147 GSK-0660

Description	GSK0660 is a potent antagonist of PPARβ and PPARδ, with IC50s of 155 nM for both isoforms.
Related Catalog	Research Areas >> Metabolic Disease
Target	PPARβ/δ:155 nM (IC50)
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].
Cell Assay	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. One hundred fifty microliters of DMSO is added to all wells and mixed thoroughly to lyse the cells and dissolve the dark blue crystals. After 10 min, the absorbance is measured at 570 nm using a microplate reader[2].
References	[1]. Shearer BG, et al. Identification and characterization of a selective peroxisome proliferator-activated receptor beta/delta (NR1C2) antagonist. Mol Endocrinol. 2008 Feb;22(2):523-9. Epub 2007 Nov 1. [2]. Zhong X, et al. Bezafibrate enhances proliferation and differentiation of osteoblastic MC3T3-E1 cells via AMPK and eNOS activation. Acta Pharmacol Sin. 2011 May;32(5):591-600. [3]. Lee WJ, et al. Activation of PPARδ attenuates neurotoxicity by inhibiting lipopolysaccharide-triggered glutamate release in BV-2 microglial cells. J Cell Biochem. 2018 Feb 1.

Density	1.4±0.1 g/cm3
Boiling Point	608.1±65.0 °C at 760 mmHg
Molecular Formula	C₁₉H₁₈N₂O₅S₂
Molecular Weight	418.487
Flash Point	321.5±34.3 °C
Exact Mass	418.065704
PSA	130.35000
LogP	2.75
Vapour Pressure	0.0±1.7 mmHg at 25°C
Index of Refraction	1.650

Personal Protective Equipment	Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
RIDADR	NONH for all modes of transport