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GW3965 hydrochloride

Cat. No. M1929

GW3965 hydrochloride Structure
Size Price Availability Quantity
10mg USD 110 In stock
50mg USD 420 In stock
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Quality Control
Biological Activity

GW3965 hydrochloride is an agonist for the liver X receptor (LXR), reduces angiotensin II-mediated pressor responses in Sprague-Dawley rats. GW3965 acts as a full agonist of hLXRα and hLXRβ (EC50 values are 190 and 30 nM respectively) in cell-based reporter gene assays. It is orally active in mice. When screened against a panel of nuclear receptors, it cross-reacted with only the pregnane X receptor (PXR). GW3965 hydrochloride displays potent antiatherogenic activity in mouse models of atherosclerosis. GW3965 dosing blunted the vasopressor effect of Ang II, which was significantly different with the 0.3 and 3 microg kg(-1) doses. GW3965 decreased Ang II-mediated vasopressor responses coincident with a trend toward reduced ATR gene expression, suggesting that LXR agonists could affect vascular reactivity. Alternate studies suggest that GW3965 hydrochloride increases apoA-I protein levels in the central nervous system independent of ABCA1. Since ABCA1 is a major regulator of cholesterol and phospholipid metabolism, GW3965 hydrochloride is a useful tool to study these cellular functions.

Protocol
Cell Experiment
Cell lines RAW264.7 cells
Preparation method Cellular Internalization of LXR Agonist
RAW264.7 cells were seeded into 24-well plates at a density of 1 × 105 cells per well 24 hours prior to the experiment. NPs encapsulating a GW3965 concentration of 1 μM were then incubated with cells for the desired time points. Afterwards, the cells were washed with PBS, followed by trypsinization and centrifugation to remove excess trypsin-EDTA. Cells were then resuspended in PBS, and cellular uptake of NPs was assessed via flow cytometry (BD LSR II, BD Bioscience, San Jose, CA). Data were analyzed using BD FACSDiva software.
Concentrations 1 μM
Incubation time 2 h
Animal Experiment
Animal models atherosclerotic lesions in Ldlr−/− mice
Formulation saline
Dosages 10mg/kg
Administration i.p.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 618.51
Formula C33H31NO3ClF3.HCl
CAS Number 405911-17-3
Purity 100.00%
Solubility DMSO ≥90 mg/mL
Storage at -20°C
References

Nanoparticles containing a liver X receptor agonist inhibit inflammation and atherosclerosis.
Zhang XQ, et al. Adv Healthc Mater. 2015 Jan 28;4(2):228-36. PMID: 25156796.

The LXR agonist GW3965 increases apoA-I protein levels in the central nervous system independent of ABCA1.
Stukas S, et al. Biochim Biophys Acta. 2012 Mar;1821(3):536-46. PMID: 21889608.

GW3965, a synthetic liver X receptor (LXR) agonist, reduces angiotensin II-mediated pressor responses in Sprague-Dawley rats.
Leik CE, et al. Br J Pharmacol. 2007 Jun;151(4):450-6. PMID: 17420776.

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Keywords: GW3965 hydrochloride supplier, Liver X Receptor, inhibitors

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