GW3965 HCl

Catalog No.S2630

GW3965 HCl Chemical Structure

Molecular Weight(MW): 618.51

GW3965 HCl is a potent, selective LXR agonist for hLXRα and hLXRβ with EC50 of 190 and 30 nM in cell-free assays, respectively.

Size Price Stock Quantity  
In DMSO USD 240 In stock
USD 97 In stock
USD 150 In stock
USD 570 In stock
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3 Customer Reviews

  • a. Western blot analysis for EpCAM, PKM2, and CK19 expression in livers from C57BL/6J mice treated with DDC for 1 week in the absence or presence of GW3965 (10 mg/kg; n = 4 per group). *P < 0.05, **P < 0.01. c Western blot analysis of p-STAT3, t-STAT3, and SOCS3 in WB-F344 cells treated with GW3965 (5 μM) or DMSO as control in response to IL-6 (50 ng/ml) treatment for 0, 0.25, 0.5, 0.75, 1, and 2 h.

    Arch Toxicol, 2017, 91(1):271-287. GW3965 HCl purchased from Selleck.

    The interaction of liver X receptor a (LXRa) and b-catenin is involved in oxLDL regulation of DKK1. Western blot analysis of cells pretreated with DMSO or GW3965 (1 μM).

    FEBS Lett, 2015, 589(1):52-8.. GW3965 HCl purchased from Selleck.

  • The effects of GW3965 on NDV infection. (A) The DF-1 cells were cultured with different concentrations of GW3965. Cell viability was determined by MTT assay at 24 h. (B) Synthetic LXR agonist GW3965 inhibited NDV infection in DF-1 cells. Cells were pretreated with GW3965 (1 μM) for 2 h, then infected with NDV (MOI = 1). GW3965 (1 μM) was continuously present during the infection. The expression level of the viral NP protein was determined by western blot. (C) The titers of the supernatant were determined by TCID50. (D) The viral gRNA in cells was detected by qRT-PCR assay.

    Arch Virol, 2016, 161(9):2491-501.. GW3965 HCl purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description GW3965 HCl is a potent, selective LXR agonist for hLXRα and hLXRβ with EC50 of 190 and 30 nM in cell-free assays, respectively.
Targets
hLXRβ [1]
(Cell-free assay)
LXRα/SRC1 LiSA [1]
(Cell-free assay)
hLXRα [1]
(Cell-free assay)
30 nM(EC50) 125 nM(EC50) 190 nM(EC50)
In vitro

GW3965 recruits the steroid receptor coactivator 1 to human LXRα with EC50 of 125 nM in a cell-free ligand-sensing assay. [1] GW3965 shows a potent antagonistic activity against hLXRα and hLXRβ in cell-based assays with EC50 of 190 nM and 30 nM, respectively. Besides, GW3965 also sows excellent selectivity over other nuclear receptors. [1] In human islets, GW3965 (1 μM) reduces expression of selected pro-inflammatory cytokines including IL-8, monocyte chemotactic protein-1 and tissue factor. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
THP1 cells MnTkSpVv[3Srb36gZZN{[Xl? MUexPEBp Ml3RTY5lfWO2aX;uJI9nKGOqb3zld5Rmem:uIHXm[ox2gCCrbjDUTHAyKGOnbHzzJIFnfGW{IEG4JIhzeyxiRVO1NF0xNjBzIN88US=> MkjvNVc1OTZ3MkG=
COS7 cells Mk\NSpVv[3Srb36gZZN{[Xl? M{jwTWFkfGm4YYTpc44hd2ZiTGjSZoV1[SClbz30doFve2[nY4Tl[EBqdiCFT2O3JINmdGy|IIfpeIghWliUYXzwbIEh[nlicnXwc5J1\XJidILhcpNi[3SrdnH0bY9vKGG|c3H5MEBGSzVyPUCuNFE2KM7:TR?= MX2xO|QyPjV{MR?=
human THP1 cells NX;5bFhNTnWwY4Tpc44h[XO|YYm= MlvXOkBp MorlRY51cWmwZnzhcY1ifG:{eTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFSKUEGgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCOUGOtd5RqdXWuYYTl[EBKVDZicILv[JVkfGmxbjDh[pRmeiB4IHjyd{BjgSCHTFnTRUwhUUN3ME2wMlAzKM7:TR?= NFHrV|cyQDhyMEe2Oy=>
mouse RAW264.7 cells MXfGeY5kfGmxbjDhd5NigQ>? NELWS4ozPCCq Mk\UTY5lfWO2aX;uJI9nKFt|SG3jbI9t\XO2ZYLvcEBm\m[udYigbY4hdW:3c3WgVmFYOjZ2LkegZ4VtdHNibH;h[IVlKHerdHigZYNmfHmuYYTl[E1NTExiYX\0[ZIhOjRiaILzMEBGSzVyPUCuNFI6KM7:TR?= MmK1NVk4OTd|MES=
human SH-SY5Y cells NVXTZo5nTnWwY4Tpc44h[XO|YYm= NVHIOmFIOjRiaB?= NEjFW5RC\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJGxZWmKndHGg[ZhxemW|c3XkJIlvKGi3bXHuJHNJNVO\NWmgZ4VtdHNiY3:teJJidnOoZXP0[YQhf2m2aDDHZYw1NUyERDDh[pRmeiB{NDDodpMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBGSzVyPUCuNVMh|ryP NEHGfHgyQTJ4NES4NS=>
human HepG2 cells M4HreGZ2dmO2aX;uJIF{e2G7 MkLPSYZn\WO2IH;uJHNTTUKSMXOg[4Vv\SCneIDy[ZN{cW:wIHnuJIh2dWGwIFjldGczKGOnbHzzMEBGSzVyPUCuNlEh|ryP M1Ozc|E5QTd|Mki4
human HuH7 cells NWnxSIpkTnWwY4Tpc44h[XO|YYm= NFHPR|lC\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJJJm[2:vYnnuZY51KEy[UnLleIEhdGmpYX7kJIJqdmSrbneg[I9u[WmwIHnuJIh2dWGwIFj1TFch[2WubIOgZ48ufHKjboPm[YN1\WRid3n0bEBnfXOnZDDHZYw1NUSERDDifUB1emGwc3HjeIl3[XSrb36gZZN{[XluIFXDOVA:OC5|MTFOwG0> MUixPFk4OzJ6OB?=
CHO cells M1vwRmZ2dmO2aX;uJIF{e2G7 NYDRNHZWSWexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBNYFJiYnX0ZUBz\WOncITvdkBmgHC{ZYPz[YQhcW5iQ1jPJINmdGy|IHL5JJJmeG:{dHXyJIF{e2G7LDDFR|UxRTBwNEGg{txO NV\Tb5U4OTdyM{SxNVk>
CHOK1 cells NYroUml5TnWwY4Tpc44h[XO|YYm= MYGyOEBp M1HvRmFod26rc4SgZYN1cX[rdImgZZQhT2GuND30ZYdo\WRiTGjSZoV1[SBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDDTG9MOSClZXzsd{Bi\nSncjCyOEBpenNiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCHQ{WwQVAvPDJizszN NFe4NGIzPTZ5N{[2OC=>
human primary hepatocytes M2j1cGZ2dmO2aX;uJIF{e2G7 M4HQUlEh|ryP MkXVTY5lfWO2aX;uJI9vKE[DUzDn[Y5mKGW6cILld5Nqd25iaX6gbJVu[W5icILpcYFzgSCqZYDheI9kgXSnczDheEAyKHWP M4DwT|E4PjZ3OEm3
human HeLa cells Mni3SpVv[3Srb36gZZN{[Xl? MorLNUDPxE1? NHj0U4FKdmS3Y4Tpc44hd2ZiTGjSZoV1[SCVVV3PfYxifGmxbjDifUBUXU2RMjDpckBpfW2jbjDI[WxiKGOnbHzzJIF1KDFidV2gZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| MW[xPFgxODd4Nx?=

... Click to View More Cell Line Experimental Data

In vivo In mice, GW3965 at a dose of 10 mg/kg upregulates ABCA1 expression 8-fold and raises circulating levels of HDL by 30% with Cmax of 12.7 μg/mL and t1/2 of 2 hours. [1] GW3965 (10mg/kg) induces expression of ABCA1 and ABCG1 and shows potent antiatherogenic activity in both LDLR−/− and apoE−/− mice. [2] In male sprague-dawley rats, GW3965 reduces Ang II-mediated increases in blood pressure and decreases vascular Ang II receptor gene expression. [3] In Glioblastoma mouse model, GW3965 results in inducible degrader of LDLR-mediated LDLR degradation, increased expression of the ABCA1 cholesterol efflux transporter, and thus potently promotes tumor cell death. [5]

Protocol

Animal Research:[1]
+ Expand
  • Animal Models: C57BL/6 mice
  • Formulation: GW3965 is dissolved in 0.5% Methyl Cellulose.
  • Dosages: ≤10 mg/kg
  • Administration: Administered via p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 16 mg/mL warmed (25.86 mM)
Water Insoluble
Ethanol 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 Information

Molecular Weight 618.51
Formula

C33H31ClF3NO3.HCl

CAS No. 405911-17-3
Storage powder
Synonyms N/A

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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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Frequently Asked Questions

  • Question 1:

    How to formulate the compound for mouse in vivo experiment?

  • Answer:

    S2630 GW3965 HCl can be dissolved in 2% DMSO/30% PEG 300/dd H2O at 10 mg/mL as a homogeneous suspension. This vehicle is suitable for oral gavage to mice.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID