GW0742

SKU: orb1300693

Description

GW0742 (GW610742) is a potent and selective PPARδ agonist, exhibiting high specificity for the human PPARδ receptor (EC50 = 1 nM) over the α and γ subtypes. This compound is a valuable research tool for studying PPARδ function in metabolic regulation, inflammation, and exercise adaptation through in vitro and in vivo experimental models.

Research Area

Metabolism Research, Molecular Biology

Images & Validation

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Key Properties

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CAS Number	317318-84-6
MW	471.49
Purity	99.85% (May vary between batches)
Formula	C₂₁H₁₇F₄NO₃S₂
SMILES	Cc1nc(sc1CSc1ccc(OCC(O)=O)c(C)c1)-c1ccc(c(F)c1)C(F)(F)F
Target	PPAR
Solubility	10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.24 mM);DMSO:60 mg/mL (127.26 mM)

Bioactivity

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Target IC50	PPARα:1.1 μM\|PPARγ:2 μM\|PPARδ:1 nM
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. Read more...
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. 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. 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. Read more...
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) Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Inhibitor, GW 0742, GW 610742, GW0742, GW-0742, GW610742, GW-610742, inhibit, PPARδ, PPARα, PPARγ, PPAR, Peroxisome proliferator-activated receptors

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Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Compound Identifiers

PubChem CID

9934458 ↗

Key Properties

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No computed properties available.

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GW0742 (orb1300693)

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MW:	446.49
Formula:	C₂₃H₂₁F₃N₂O₂S

Purity:	>98% (HPLC)
CAS Number:	317318-84-6
MW:	471.5
Formula:	C₂₁H₁₇F₄NO₃S₂

GW0742

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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