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    GW3965 HCl
    GW3965 HCl

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1852
    CAS #: 405911-17-3 Purity ≥98%

    Description: GW3965 HCl is a novel, potent, selective LXR (liver X receptor) agonist for hLXRα and hLXRβ. In cell-based reporter gene assays, GW3965 plays as a full agonist on hLXRα and hLXRβ with EC50 of 190 and 30 nM, respectively. GW3965 suppresses the production of pro-inflammatory cytokines by murine mast cells. GW3965 improves recovery from mild repetitive traumatic brain injury in mice partly through apolipoprotein E. GW3965 reduces tissue factor production and inflammatory responses in human islets in vitro. GW3965 dose-dependently regulates lps-mediated liver injury and modulates posttranscriptional TNF-alpha production and p38 mitogen-activated protein kinase activation in liver macrophages.

    References: J Med Chem. 2002 May 9;45(10):1963-6; Proc Natl Acad Sci U S A. 2002 May 28;99(11):7604-9.

    Related CAS#: 405911-09-3 (free); 405911-17-3 (HCl)

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    Molecular Weight (MW)618.51 
    FormulaC33H31ClF3NO3.HCl 
    CAS No.405911-17-3 HCI
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 16 mg/mL (25.9 mM)          
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other infoChemical Name: 2-(3-(3-((2-chloro-3-(trifluoromethyl)benzyl)(2,2-diphenylethyl)amino)propoxy)phenyl)acetic acid hydrochloride
    InChi Key: NMPUWJFHNOUNQU-UHFFFAOYSA-N
    InChi Code: InChI=1S/C33H31ClF3NO3.ClH/c34-32-27(15-8-17-30(32)33(35,36)37)22-38(18-9-19-41-28-16-7-10-24(20-28)21-31(39)40)23-29(25-11-3-1-4-12-25)26-13-5-2-6-14-26;/h1-8,10-17,20,29H,9,18-19,21-23H2,(H,39,40);1H
    SMILES Code: OC(CC1=CC(OCCCN(CC2=C(Cl)C(C(F)(F)F)=CC=C2)CC(C3=CC=CC=C3)C4=CC=CC=C4)=CC=C1)=O.Cl
    SynonymsGW-3965; GW3965; GW 3965; GW-3965 HCl; GW-3965 hydrochloride


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    In Vitro

    In vitro activity: GW3965 recruits the steroid receptor coactivator 1 to human LXRα with EC50 of 125 nM in a cell-free ligand-sensing assay. 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. In human islets, GW3965 (1 μM) reduces expression of selected pro-inflammatory cytokines including IL-8, monocyte chemotactic protein-1 and tissue factor.


    Kinase Assay: GW3965 hydrochloride is a potent and selective liver X receptor (LXR) agonist with EC50s of 190 and 30 nM for hLXRα and hLXRβ , respectively.


    Cell Assay: Cells are seeded in 96 wells and are treated after 24 hours with different drugs indicated in each experiment in medium containing 1% FBS or lipoprotein deficient serum. Relative proliferation is determined using Cell Proliferation Assay Kit. Cells are incubated 1.5 hrs after adding tetrazolium salt WST-1 [2-(4-iodophenyl)-3- (4-nitrophenyl)-5-(2, 4-disulfo-phenyl)-2H-tetrazolium, monosodium salt] at 5% CO2, 37ºC and the absorbance of the treated and untreated cells are measured using a microplate reader at 420 to 480 nm. Cells seeded in 12 well plates are counted using a hemocytometer, and dead cells are assessed using trypan blue exclusion assays.

    In VivoIn 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. GW3965 (10mg/kg) induces expression of ABCA1 and ABCG1 and shows potent antiatherogenic activity in both LDLR−/− and apoE−/− mice. In male sprague-dawley rats, GW3965 reduces Ang II-mediated increases in blood pressure and decreases vascular Ang II receptor gene expression. 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. 
    Animal modelC57BL/6 mice 
    Formulation & DosageDissolved in 0.5% Methyl Cellulose;  ≤10 mg/kg; oral gavage
    ReferencesJ Med Chem. 2002 May 9;45(10):1963-6; Proc Natl Acad Sci U S A. 2002 May 28;99(11):7604-9. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    GW3965 HCl

    GW3965 inhibits the development of aortic lesions in LDLR−/− mice. Proc Natl Acad Sci U S A. 2002 May 28;99(11):7604-9.
     

    GW3965 HCl

    En face and aortic root section analysis of atherosclerosis in LDLR−/− mice. Proc Natl Acad Sci U S A. 2002 May 28;99(11):7604-9.
     

    GW3965 HCl

    Regulation of LXR target gene expression by GW3965 in liver and intestine in apoE−/− mice. ApoE−/− mice (five animals per group) were treated for the indicated time with either vehicle or 10 mpk GW3965. Proc Natl Acad Sci U S A. 2002 May 28;99(11):7604-9.


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