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GW3965 hydrochloride

Catalog No. T6310 CAS 405911-17-3

Synonyms: GW3965 HCl

GW3965 hydrochloride (GW3965 HCl) is an effective and specific LXR agonist for hLXRα/β (EC50: 190/30 nM).

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GW3965 hydrochloride, CAS 405911-17-3

Pack Size	Availability	Price/USD
2 mg	In stock	$ 35.00
5 mg	In stock	$ 57.00
10 mg	In stock	$ 90.00
25 mg	In stock	$ 198.00
50 mg	In stock	$ 378.00
100 mg	In stock	$ 562.00
500 mg	In stock	$ 1,230.00
1 mL * 10 mM (in DMSO)	In stock	$ 79.00

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Purity: 99.75%

Purity: 99.51%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	GW3965 hydrochloride (GW3965 HCl) is an effective and specific LXR agonist for hLXRα/β (EC50: 190/30 nM).
Targets&IC50	LXRα (human):190 nM(EC50), LXRβ (human):30 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 (10 mg/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]
Kinase Assay	Steady-state drug accumulation assay: AuxB1 and CHrB30 cells are grown to confluency in 12-well (24 mm) tissue culture dishes and the steady-state accumulation of [3H]-vinblastine is measured. Accumulation is initiated by the addition of 0.1 μ Ci [3H]-vinblastine and unlabelled vinblastine to a final concentration of 100 nM . The accumulation of [3H]-paclitaxel is measured using 0.1 μ Ci [3H]-paclitaxel and unlabelled drug to a final concentration of 1 μM . Cells are incubated in a reaction volume of 1 mL for 60 min at 37 ℃ under 5% CO2 in order to reach steady-state. The effect of the modulators XR9576 on [3H]-ligand accumulation is investigated in the concentration range 10-9 - 10-6 M. Modulators are added from a DMSO stock giving a final solvent concentration of 0.2 % (v/v). Following cell harvesting, accumulated drug is measured by liquid scintillation counting and normalized for cell protein content. Plots of amount accumulated as a function of modulator concentration are fitted with the general dose-response equation: Y={(a-b)/(1+(X/c)d)}+b Where: Y=response; a=initial response; b=final response; c=EC50 concentration; d=slope value; X=drug concentration.
Cell Research	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.

Synonyms	GW3965 HCl
Molecular Weight	618.51
Formula	C33H31ClF3NO3·HCl
CAS No.	405911-17-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 61.9 mg/mL (100 mM)

Ethanol: 12.4 mg/mL (20 mM)

References and Literature

1. Collins JL, et al. J Med Chem. 2002, 45(10), 1963-1966. 2. Joseph SB, et al. Proc Natl Acad Sci U S A. 2002, 99(11), 7604-7609. 3. Leik CE, et al. Br J Pharmacol. 2007, 151(4), 450-456. 4. Scholz H, et al. Diabetologia. 2009, 52(7), 1352-1362. 5. Guo D, et al. Cancer Discov. 2011, 1(5), 442-456.

Citations

1. Liu Y, Wang Z, Jin H, et al.Squalene-epoxidase-catalyzed 24 (S), 25-epoxycholesterol synthesis promotes trained-immunity-mediated antitumor activity.Cell Reports.2024, 43(4).

Related compound libraries

This product is contained In the following compound libraries：

Metabolism Compound Library Bioactive Compound Library Nuclear Receptor Compound Library Preclinical Compound Library Lipid Metabolism Compound Library Anti-Metabolism Disease Compound Library Fluorochemical Library Immunology/Inflammation Compound Library Bioactive Compounds Library Max NO PAINS Compound Library

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Keywords

GW3965 hydrochloride 405911-17-3 Metabolism Liver X Receptor GW-3965 GW3965 HCl Liver X receptor GW-3965 hydrochloride Inhibitor GW3965 inhibit GW3965 Hydrochloride LXR GW-3965 Hydrochloride GW 3965 GW 3965 Hydrochloride inhibitor

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