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GW0742

Catalog No. T6524 CAS 317318-84-6

Synonyms: GW610742

GW0742 (GW610742) is an effective and specific PPARδ agonist (EC50: 1 nM/1.1 μM/2 μM, for human PPARδ/α/γ).

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GW0742, CAS 317318-84-6

Pack Size	Availability	Price/USD
5 mg	In stock	$ 43.00
10 mg	In stock	$ 68.00
25 mg	In stock	$ 127.00
50 mg	In stock	$ 231.00
100 mg	In stock	$ 401.00
500 mg	In stock	$ 953.00
1 mL * 10 mM (in DMSO)	In stock	$ 48.00

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Purity: 99.85%

Purity: 99.83%

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Description	GW0742 (GW610742) is an effective and specific PPARδ agonist (EC50: 1 nM/1.1 μM/2 μM, for human PPARδ/α/γ).
Targets&IC50	PPARα:1.1 μM, PPARγ:2 μM, PPARδ:1 nM
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] GW0742 (0.2 μM and 1 μM) significant increases in reporter activity of PPARβ/δ in N/TERT-1 keratinocytes. GW0742 (1 μM) results in significant inhibition in the average number of N/TERT-1 keratinocytes. GW0742 (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. GW0742 (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. GW0742 (1 μM) results in significantly reduced phosphorylation of retinoblastoma (Rb) and a significantly lower level of p42/44 ERK in N/TERT-1 cells. GW0742 (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] GW0742 at 100 μM produces a significant reduction in low-KCl-induced neuronal cell death in cerebellar granule neurons. GW0742 at 100 μM induces a pronounced increase in cell death as measured by LDH release after 48 hr of incubation. GW0742 at 100 μM produces a pronounced increase in c-Jun expression at 6 hours in cerebellar granule neuron cultures. GW0742 at 100 μM increases PPARα-mediated transactivation dependent on the presence of 1.5% BSA in MCF-7 cells. [3]
In vivo	GW0742-treatment (0.3 mg/Kg, 10 % DMSO, i.p.) has therapeutic effects on pulmonary damage, decreasing many inflammatory and apoptotic parameters detected by measurement of 1) cytokine production; 2) leukocyte accumulation, indirectly measured as decrease of myeloperoxidase (MPO) activity; 3) IkBα degradation and NF-kB nuclear translocation; 4) ERK phosphorylation; 5) stress oxidative by NO formation due to iNOS expression; 6) nitrotyrosine and PAR localization; 7) the degree of apoptosis, evaluated by Bax and Bcl-2 balance, FAS ligand expression and TUNEL staining. Taken together, GW0742 reduces the lung injury and inflammation due to the intratracheal BLEO--instillation in mice.
Cell Research	N/TERT-1 keratinocytes are seeded onto 6-well tissue culture dishes at 3×104 cells per well in Ker-SFM. Twenty-four hours later, cell number is measured with a Z1 coulter particle counter to determine plating efficiency (Day 0). For the remaining cells, medium is changed to Ker-SFM/DF-K, and cells are treated in triplicate with 0.1% DMSO, 0.1 μM or 1 μM GW0742. Cell number is determined at daily intervals, and the remaining cells are retreated with fresh media and treatment each day for up to 6 days.(Only for Reference)

Synonyms	GW610742
Molecular Weight	471.49
Formula	C21H17F4NO3S2
CAS No.	317318-84-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 48.5 mg/mL(100 mM)

References and Literature

1. Sznaidman ML, et al. Bioorg Med Chem Lett, 2003, 13(9), 1517-1521. 2. Burdick AD, et al. Cell Signal, 2007, 19(6), 1163-1171. 3. Smith SA, et al. J Neurosci Res, 2004, 77(2), 240-249. 4. Briand F, et al. Clin Transl Sci, 2009, 2(2), 127-133. 5. Haskova Z, et al. Inflamm Res, 2008, 57(7), 314-321.

Citations

1. Dou X, Huo T, Liu Y, et al.Discovery of novel and selective farnesoid X receptor antagonists through structure-based virtual screening, preliminary structure-activity relationship study, and biological evaluation.European Journal of Medicinal Chemistry.2024: 116323.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Neurodegenerative Disease Compound Library Anti-Cancer Active Compound Library Anti-Obesity Compound Library Glycometabolism Compound Library Mitochondria-Targeted Compound Library Anti-Breast Cancer Compound Library Bioactive Compounds Library Max DNA Damage & Repair Compound Library Anti-Pancreatic Cancer Compound Library Metabolism Compound Library

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Keywords

GW0742 317318-84-6 DNA Damage/DNA Repair Metabolism PPAR inhibit GW610742 GW 610742 Inhibitor GW 0742 Peroxisome proliferator-activated receptors GW-0742 GW-610742 inhibitor

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