GW0742

Catalog No.S8020

For research use only.

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

GW0742 Chemical Structure

CAS No. 317318-84-6

Selleck's GW0742 has been cited by 6 Publications

3 Customer Reviews

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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.
Features Both GW0742 and L-165041 activate PPARβ, but not PPARγ or PPARα in platelets.
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CV-1 cells NVLR[IVkTnWwY4Tpc44h[XO|YYm= M3nM[lI1KGh? NYC3VmpWSWexbnnzeEBi[3Srdnn0fUBifCCvb4Xz[UBRWEGULXHsdIhiKGW6cILld5Nm\CCrbjDh[pJq[2GwIHfy[YVvKG2xbnvlfUBEXi1zIHPlcIx{KGGodHXyJFI1KGi{czDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[Xl? NGLCfZYzOTB5NESzNi=>
HEK293 cells NEjkO3dHfW6ldHnvckBie3OjeR?= MXrUdoFve2GldHn2ZZRqd25ib3[gVHBCWmSnbIThJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKEiHS{K5N{Bk\WyuczDjc{11emGwc3\lZ5Rm\CC5aYToJHBFUzRvUGDSSUBjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYm= M2Pub|I{Ojd|NUG5
C2C12 cells M{P1cmZ2dmO2aX;uJIF{e2G7 M1i3OVQh\GG7cx?= NFnrdYVC\2:waYP0JIFkfGm4aYT5JIF1KFCSQWLk[Yx1[SCrbjDtc5V{\SCFMlOxNkBk\WyuczDhd5Nme3OnZDDhd{B2eHKnZ4XsZZRqd25ib3[gWGZCVSCpZX7lJIV5eHKnc4Ppc44h[W[2ZYKgOEBl[Xm|IHL5JJJm[WxidHnt[UBRS1JiYX7hcJl{cXN? NEHnUIkzOzJ5M{WxPS=>
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]

Protocol (from reference)

Cell Research:[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 Research:[4]
  • Animal Models: Wild-type C57BL/6 female mice
  • Dosages: 10 mg/kg
  • Administration: Supplemented chow diet

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2% DMSO+40% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.

3mg/mL

Chemical Information

Molecular Weight 471.49
Formula

C21H17F4NO3S2

CAS No. 317318-84-6
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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