Home Metabolism PPAR agonist GW0742

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GW0742 PPAR agonist

Cat.No.S8020

GW0742 is a potent and highly selective PPARβ/δ agonist, with IC50 of 1 nM, with 1000-fold selectivity over hPPARα and hPPARγ.
GW0742 PPAR agonist Chemical Structure

Chemical Structure

Molecular Weight: 471.49

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Quality Control

Batch: S802001 DMSO]94 mg/mL]false]Ethanol]44 mg/mL]false]Water]Insoluble]false Purity: 99.99%
99.99

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CV-1 cells Function assay 24 h Agonist activity at mouse PPAR-alpha expressed in african green monkey CV-1 cells after 24 hrs by luciferase reporter gene assay
HEK293 cells Function assay Transactivation of PPARdelta (unknown origin) expressed in HEK293 cells co-transfected with PDK4-PPRE by luciferase reporter gene assay
C2C12 cells Function assay 4 days Agonist activity at PPARdelta in mouse C2C12 cells assessed as upregulation of TFAM gene expression after 4 days by real time PCR analysis
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight 471.49 Formula

C21H17F4NO3S2

 Storage (From the date of receipt)
CAS No. 317318-84-6 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=C(C=CC(=C1)SCC2=C(N=C(S2)C3=CC(=C(C=C3)C(F)(F)F)F)C)OCC(=O)O

Solubility

In vitro
Batch:

DMSO : 94 mg/mL ( (199.36 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 44 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Mechanism of Action

Features
Both GW0742 and L-165041 activate PPARβ, but not PPARγ or PPARα in platelets.
Targets/IC50/Ki
PPARδ [1]
1 nM(EC50)
In vitro
GW0742 shows activity aganist hPPARα, hPPARγ and hPPARδ with EC50 of 1.1 μM, 2 μM and 1 nM, respectively, in cell based transactivation assay. [1] This compound (0.2 μM and 1 μM) significant increases in reporter activity of PPARβ/δ in N/TERT-1 keratinocytes. It (1 μM) results in significant inhibition in the average number of N/TERT-1 keratinocytes. The chemical (1 μM) results in an increase in the number of cells in the G1 phase and a decrease in the number of cells in the S phase. It (1 μM) causes a significant increase in the mRNA encoding ADRP, a known PPARβ/δ target gene, in N/TERT-1 keratinocytes as well as mouse primary keratinocytes. This agent (1 μM) results in significantly reduced phosphorylation of retinoblastoma (Rb) and a significantly lower level of p42/44 ERK in N/TERT-1 cells. It (1 μM) leads to an increase in the mRNA encoding a number of known markers of terminal differentiation including TG-I, SPR1A, K10 and involucrin. [2] This compound at 100 μM produces a significant reduction in low-KCl-induced neuronal cell death in cerebellar granule neurons. It at 100 μM induces a pronounced increase in cell death as measured by LDH release after 48 hr of incubation. The chemical at 100 μM produces a pronounced increase in c-Jun expression at 6 hours in cerebellar granule neuron cultures. It at 100 μM increases PPARα-mediated transactivation dependent on the presence of 1.5% BSA in MCF-7 cells. [3]
In vivo
GW0742 (10 mg/kg) promotes reverse cholesterol transport in C57BL6/J mice. This compound (10 mg/kg) increases the fecal excretion of HDLderived cholesterol despite no effect on HDL cholesterol catabolism in C57BL6/J mice. It decreases NPC1L1 mRNA expression in the small intestine of mice. [4] This chemical (30 mg/kg), prior to induction of LPS-mediated pulmonary inflammation, results in a significant decrease in leukocyte recruitment into the pulmonary space in Male BALB/c mice. It (30 mg/kg) significantly decreases protein and mRNA levels of the pro-inflammatory cytokines IL-6, IL-1beta and TNFalpha in Bronchial alveolar lavage fluid of mice. [5]
References
  • https://pubmed.ncbi.nlm.nih.gov/20169010/
  • https://pubmed.ncbi.nlm.nih.gov/18622687/

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