GW0742X

GW0742X - Names and Identifiers

Name	GW0742
Synonyms	GW0742 GW0742X GW610742 GW 0742X GW 610742 GWdelta0742 GWdelta 0742 2-(4-(((2-(3-Fluoro-4-(trifluoromethyl)phenyl)-4-methylthiazol-5-yl)methyl)thio)-2-methylpheno 2-(4-(((2-(3-Fluoro-4-(trifluoromethyl)phenyl)-4-methylthiazol-5-yl)methyl)thio)-2-methylphenoxy) 4-[2-(3-FLUORO-4-TRIFLUOROMETHYL-PHENYL)-4-METHYL-THIAZOL-5-YLMETHYLSULFANYL]-2-METHYL-PHENOXY-ACETIC ACID [4-[[[2-[3-FLUORO-4-(TRIFLUOROMETHYL)PHENYL]-4-METHYL-5-THIAZOLYL]METHYL]THIO]-2-METHYLPHENOXY]ACETIC ACID
CAS	317318-84-6
EINECS	1532714-185-1
InChIKey	HWVNEWGKWRGSRK-UHFFFAOYSA-N

GW0742X - Physico-chemical Properties

Molecular Formula	C21H17F4NO3S2
Molar Mass	471.49
Density	1.46±0.1 g/cm3(Predicted)
Melting Point	134.5-135.5 °C
Boling Point	591.5±60.0 °C(Predicted)
Solubility	DMSO: >5mg/mL
Appearance	solid
Color	white
pKa	3.17±0.10(Predicted)
Storage Condition	2-8°C
MDL	MFCD07369423
Physical and Chemical Properties	Bioactive GW0742 is a potent, selective PPAR β/δ agonist with an IC50 of 1 nM, which is 1000-fold more selective than hPPAR α and hPPAR γ.
Use	Uses GW0742 is a small molecule agonist of the human peroxisome proliferator-activated receptor δ(PPAR δ). It shows an EC50 of 1.1 nM for PPAR δ, which is 100-fold more selective than other human subtypes.
In vitro study	In basic cell transcription experiments, GW0742 effectively acted on hPPAR α,hPPAR γ, and hPPAR δ with EC50 of 1.1 μm, 2 μm, and 1 nM, respectively. GW0742 (0.2 μm and 1 μm) significantly increased PPAR β/δ activity in N/TERT-1 keratinocytes. GW0742 (1 μm) significantly inhibited the average cell number of N/TERT-1 keratinocytes. GW0742 (1 M) increased the number of cells in G1 phase, decreased the number of cells in S phase. GW0742 (1 μm) acts on N/TERT-1 keratinocytes and mouse primary keratinocytes to significantly increase mRNA-encoded ADRP, a PPAR β/δ target gene. GW0742 (1 μm) significantly reduced phosphorylation of retinoblastoma (Rb) and p42/44 ERK levels in N/TERT-1 cells. 100 μm GW0742 significantly reduced low KCl-induced neuronal cell death in cerebellar granule neurons. By measuring LDH release, it was observed that 100 μm GW0742 significantly enhanced cell death. Treatment of cerebellar granule neuron medium with 100 μm GW0742 for 6 hours significantly enhanced c-Jun expression. 100 μm GW0742 acts on MCF-7 cells to increase PPARα-mediated transcription in the presence of 1.5% BSA.
In vivo study	GW0742 (10 mg/kg) treatment of C57BL6/J mice promoted reverse cholesterol transport. GW0742 (10 mg/kg) treatment of C57BL6/J mice promoted fecal excretion of HDL cholesterol, although there was no effect on HDL cholesterol metabolism. GW0742 acts on the small intestine of mice to reduce the expression of NPC1L1 mRNA. GW0742 (30 mg/kg) treatment of Male BALB/c mice significantly reduced leukocyte recruitment into the lung space prior to induction of LPS-mediated lung inflammation. GW0742 (30 mg/kg) treatment of mouse bronchoalveolar lavage fluid significantly reduced the protein and mRNA levels of proinflammatory cytokines IL-6,IL-1β and TNF-α.