GW0742

Catalog 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.

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GW0742 Chemical Structure

GW0742 Chemical Structure
Molecular Weight: 471.49

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Quality Control & MSDS

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Product Description

Biological Activity

Description GW0742 is a potent and highly selective PPARβ/δ agonist, with IC50 of 1 nM, with 1000-fold selectivity over hPPARα and hPPARγ.
Targets PPARδ [1]
IC50 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 (10 mg/kg) promotes reverse cholesterol transport in C57BL6/J mice. GW0742 (10 mg/kg) increases the fecal excretion of HDLderived cholesterol despite no effect on HDL cholesterol catabolism in C57BL6/J mice. GW0742 decreases NPC1L1 mRNA expression in the small intestine of mice. [4] GW0742 (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. GW0742 (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]
Features Both GW0742 and L-165041 activate PPARβ, but not PPARγ or PPARα in platelets.

Protocol(Only for Reference)

Cell Assay: [2]

Cell lines N/TERT-1 keratinocytes
Concentrations ~1 μM
Incubation Time 6 days
Method 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.

Animal Study: [4]

Animal Models Wild-type C57BL/6 female mice
Formulation Saline
Dosages 10 mg/kg
Administration Supplemented chow diet

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[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.

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Chemical Information

Download GW0742 SDF
Molecular Weight (MW) 471.49
Formula

C21H17F4NO3S2

CAS No. 317318-84-6
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 94 mg/mL (199.36 mM)
Ethanol 44 mg/mL (93.32 mM)
Water <1 mg/mL (<1 mM)
In vivo 30% propylene glycol, 5% Tween 80, 65% D5W 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name Acetic acid, 2-[4-[[[2-[3-fluoro-4-(trifluoromethyl)phenyl]-4-methyl-5-thiazolyl]methyl]thio]-2-methylphenoxy]-

Tech Support

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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