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GW0742

Name: GW0742
Brand: Selleck Chemicals
SKU: S8020
Rating: 5 (6 reviews)

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.

CAS No. 317318-84-6

Selleck's GW0742 has been cited by 6 Publications

3 Customer Reviews

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PPAR Signaling Pathway Map

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=>

Click to View More Cell Line Experimental Data

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

References

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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. Click to purchase: PEG300 Tween 80	3mg/mL

Chemical Information

Molecular Weight	471.49
Formula	C₂₁H₁₇F₄NO₃S₂
CAS No.	317318-84-6
Storage	3 years	-20°C	powder
Storage	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

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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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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.
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Molarity Calculator

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