GW3965 HCl

Alias: GW-3965;GW-3965 HCl;GW3965; GW 3965; GW-3965 hydrochloride
Cat No.:V1852 Purity: ≥98%
GW3965 (GW-3965) HCl, the hydrochloride salt ofGW3965, is a novel, potent, selective LXR (liver X receptor) agonist for hLXRα and hLXRβ with potential anti-inflammatory activity.
GW3965 HCl Chemical Structure CAS No.: 405911-17-3
Product category: LXR
This product is for research use only, not for human use. We do not sell to patients.
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Other Forms of GW3965 HCl:

  • GW3965
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Purity: ≥98%

Product Description

GW3965 (GW-3965) HCl, the hydrochloride salt of GW3965, is a novel, potent, selective LXR (liver X receptor) agonist for hLXRα and hLXRβ with potential anti-inflammatory activity. 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.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
In vitro, GW3965 hydrochloride induces GBM cell death with increased effectiveness in tumor cells that express EGFRvIII. GW3965 hydrochloride decreases LDLR levels while upregulating the expression of the E3 ubiquitin ligase IDOL and the cholesterol transporter gene ABCA1[2]. Platelet aggregation and calcium mobilization induced by collagen or CRP are inhibited by LXR ligands. When platelets are activated with 1 μg/mL CRP, GW3965 hydrochloride (1 or 5 μM) exhibits a slight inhibitory effect on fibrinogen binding and P-selectin exposure. GW3965 hydrochloride (10 μM) and T0901317 (40 μM) at greater concentrations, however, decrease the amounts of fibrinogen and P-selectin on the platelet surface[3].
ln Vivo
The CNS of non-pathological animals does not experience the elevation in neuroactive steroids that GW3965 hydrochloride causes in the spinal cord, cerebellum, and cerebral cortex of STZ-rats. When diabetic animals are treated with GW3965 hydrochloride, their spinal cords express more myelin basic protein and have higher levels of dihydroprogesterone[1]. In vivo, GW3965 hydrochloride (40 mg/kg, po) significantly increases GBM cell death by a factor of 25 and robustly promotes ABCA1 and decreases LDLR expression[2]. Additionally, it inhibits tumor growth by 59%. In vivo bleeding duration is prolonged and platelet thrombus development is regulated by GW3965 hydrochloride (2 mg/kg, IV)[3].
Animal Protocol
Dissolved in 0.5% Methyl Cellulose; ≤10 mg/kg; oral gavage [1]
C57BL/6 mice
References
[1]. Mitro, Nico., et al. LXR and TSPO as new therapeutic targets to increase the levels of neuroactive steroids in the central nervous system of diabetic animals. Neurochemistry International (2012), 60(6), 616-621.
[2]. Guo, Deliang., et al. An LXR Agonist Promotes Glioblastoma Cell Death through Inhibition of an EGFR/AKT/SREBP-1/LDLR-Dependent Pathway. Cancer Discovery (2011), 1(5), 442-456.
[3]. Spyridon, Michael., et al. LXR as a novel antithrombotic target. Blood (2011), 117(21), 5751-5761.
[4]. Collins JL, et al. Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines. J Med Chem. 2002 May 9;45(10):1963-6
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C33H31CLF3NO3.HCL
Molecular Weight
618.51
CAS #
405911-17-3
SMILES
ClC1C(C(F)(F)F)=C([H])C([H])=C([H])C=1C([H])([H])N(C([H])([H])C([H])([H])C([H])([H])OC1=C([H])C([H])=C([H])C(C([H])([H])C(=O)O[H])=C1[H])C([H])([H])C([H])(C1C([H])=C([H])C([H])=C([H])C=1[H])C1C([H])=C([H])C([H])=C([H])C=1[H].Cl[H]
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
Chemical Name
2-(3-(3-((2-chloro-3-(trifluoromethyl)benzyl)(2,2-diphenylethyl)amino)propoxy)phenyl)acetic acid hydrochloride
Synonyms
GW-3965;GW-3965 HCl;GW3965; GW 3965; GW-3965 hydrochloride
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO:16 mg/mL (25.9 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.6168 mL 8.0839 mL 16.1679 mL
5 mM 0.3234 mL 1.6168 mL 3.2336 mL
10 mM 0.1617 mL 0.8084 mL 1.6168 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
  • 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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