1014691-61-2
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
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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 | |
| 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 |
| 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 |