GW3965 HCl

Catalog No.S2630 Batch:S263007

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Technical Data

Formula

C33H31ClF3NO3.HCl
Molecular Weight 618.51 CAS No. 405911-17-3
Solubility (25°C)* In vitro DMSO 33 mg/mL (53.35 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
0.8mg/ml Taking the 1 mL working solution as an example, add 50 μL of clarified DMSO stock solution of 16 mg/ml to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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]
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 (from reference)

Animal Study:

[1]
  • Animal Models

    C57BL/6 mice

  • Dosages

    ≤10 mg/kg

  • Administration

    Administered via p.o.

Customer Product Validation

, , FEBS Lett, 2015, 589(1):52-8.

Data from [Data independently produced by , , Arch Toxicol, 2017, 91(1):271-287]

Data from [Data independently produced by , , Exp Neurol, 2018, 304:21-29]

Data from [Data independently produced by , , J Cell Biochem, 2016, 117(10):2272-80]

Selleck's GW3965 HCl has been cited by 43 publications

Host-to-graft propagation of inoculated α-synuclein into transplanted human induced pluripotent stem cell-derived midbrain dopaminergic neurons [ Regen Ther, 2024, 25:229-237] PubMed: 38283940
Restoration of lipid homeostasis between TG and PE by the LXRα-ATGL/EPT1 axis ameliorates hepatosteatosis [ Cell Death Dis, 2023, 14(2):85] PubMed: 36746922
Activation of liver X receptors suppresses the abundance and osteoclastogenic potential of osteoclast precursors and periodontal bone loss [ Mol Oral Microbiol, 2023, 10.1111/omi.12447] PubMed: 38108557
Expression and role of nicotinic acetylcholine receptors during midbrain dopaminergic neuron differentiation from human induced pluripotent stem cells [ Neuropsychopharmacol Rep, 2023, 10.1002/npr2.12361] PubMed: 37366076
Oridonin alleviates hyperbilirubinemia through activating LXRα-UGT1A1 axis [ Pharmacol Res, 2022, 178:106188] PubMed: 35338002
Integrated Analysis Highlights the Immunosuppressive Role of TREM2+ Macrophages in Hepatocellular Carcinoma [ Front Immunol, 2022, 13:848367] PubMed: 35359989
Liver X receptor-agonist treatment rescues degeneration in a Drosophila model of hereditary spastic paraplegia [ Acta Neuropathol Commun, 2022, 10(1):40] PubMed: 35346366
Activation of LXRs Reduces Oxysterol Lipotoxicity in RPE Cells by Promoting Mitochondrial Function [ Nutrients, 2022, 14(12)2473] PubMed: 35745203
Activation of liver X receptors protects oligodendrocytes in CA3 of stress-induced mice [ Front Pharmacol, 2022, 13:936045] PubMed: 35959443
Deficiency of proline/serine-rich coiled-coil protein 1 (PSRC1) accelerates trimethylamine N-oxide-induced atherosclerosis in ApoE-/- mice [ J Mol Cell Cardiol, 2022, 170:60-74] PubMed: 35690006

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.