GW0742

Catalog No.S8020 Batch:S802001

Technical Data

Formula

C₂₁H₁₇F₄NO₃S₂

Molecular Weight

471.49

CAS No.

317318-84-6

Solubility (25°C)*

In vitro

DMSO

94 mg/mL (199.36 mM)

Ethanol

44 mg/mL (93.32 mM)

Water

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution

2%DMSO 1 40%PEG300 2 2%Tween80 3 56%ddH2O

3.0mg/ml

Taking the 1 mL working solution as an example, add 20 μL of 150 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 20 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 560 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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]

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] 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 (from 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 Dosages 10 mg/kg Administration Supplemented chow diet

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
Dosages
10 mg/kg
Administration
Supplemented chow diet

References

+ Expand

Customer Product Validation

: Data from [Data independently produced by , , Neuropharmacology, 2016, 113(Pt A):396-406. ]

: Data from [Data independently produced by , , Sci Rep, 2017, 7:45234]

: Data from [Data independently produced by , , Lab Invest, 2016, 96(2):218-29]

Selleck's GW0742 has been cited by 9 publications

PPAR-γ agonists reactivate the ALDOC-NR2F1 axis to enhance sensitivity to temozolomide and suppress glioblastoma progression [ Cell Commun Signal, 2024, 22(1):266]	PubMed: 38741139
A drug repurposing study identifies novel FOXM1 inhibitors with in vitro activity against breast cancer cells [ Med Oncol, 2024, 41(8):188]	PubMed: 38918225
SWIM domain protein ZSWIM4 is required for JAK2 inhibition resistance in breast cancer [ Life Sci, 2021, 279:119696]	PubMed: 34102191
Vascular PPARβ/δ Promotes Tumor Angiogenesis and Progression. [ Cells, 2019, 8(12)]	PubMed: 31842402
PPAR δ inhibition protects against palmitic acid-LPS induced lipidosis and injury in cultured hepatocyte L02 cell. [ Int J Med Sci, 2019, 16(12):1593-1603]	PubMed: 31839747
PPAR δ inhibition protects against palmitic acid-LPS induced lipidosis and injury in cultured hepatocyte L02 cell [ Int J Med Sci, 2019, 16(12):1593-1603]	PubMed: 31839747
PPARβ/δ, a Novel Regulator for Vascular Smooth Muscle Cells Phenotypic Modulation and Vascular Remodeling after Subarachnoid Hemorrhage in Rats. [Zhang H, et al. Sci Rep, 2017, 7:45234]	PubMed: 28327554
WNT/β-catenin signaling regulates cigarette smoke-induced airway inflammation via the PPARδ/p38 pathway. [Guo L, et al. Lab Invest, 2016, 96(2):218-29]	PubMed: 26322419
PPARβ/δ activation protects against corticosterone-induced ER stress in astrocytes by inhibiting the CpG hypermethylation of MicroRNA-181a [Ji J, et al. Neuropharmacology, 2016, 10.1016/j.neuropharm.2016.10.022]	PubMed: 27789312

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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