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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	NYrEdVYzTnWwY4Tpc44h[XO\|YYm=	MX6yOEBp	MWfB[49vcXO2IHHjeIl3cXS7IHH0JI1wfXOnIGDQRXIu[WyyaHGg[ZhxemW\|c3XkJIlvKGGocnnjZY4h\3KnZX6gcY9vc2W7IFPWMVEh[2WubIOgZYZ1\XJiMkSgbJJ{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfS=>	M4jod\|IyODd2NEOy
HEK293 cells	MkmxSpVv[3Srb36gZZN{[Xl?		MXjUdoFve2GldHn2ZZRqd25ib3[gVHBCWmSnbIThJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW\|c3XkJIlvKEiHS{K5N{Bk\WyuczDjc{11emGwc3\lZ5Rm\CC5aYToJHBFUzRvUGDSSUBjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO\|YYm=	M1nydFI{Ojd\|NUG5
C2C12 cells	NILoZpVHfW6ldHnvckBie3OjeR?=	MkLHOEBl[Xm\|	NWPnTJNTSWexbnnzeEBi[3Srdnn0fUBifCCSUFHS[IVtfGFiaX6gcY92e2ViQ{LDNVIh[2WubIOgZZN{\XO\|ZXSgZZMhfXC{ZXf1cIF1cW:wIH;mJHRHSU1iZ3Xu[UBmgHC{ZYPzbY9vKGGodHXyJFQh\GG7czDifUBz\WGuIITpcYUhWEOUIHHuZYx6e2m\|	NYL3SYlLOjN{N{O1NVk>

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	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 (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:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

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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Dilution Calculator Molecular Weight Calculator

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