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GW3965 hydrochloride

Cat. No. M1929
GW3965 hydrochloride Structure

GW3965 HCl

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
2mg USD 38  USD38 In stock
5mg USD 68  USD68 In stock
10mg USD 102  USD102 In stock
50mg USD 400  USD400 In stock
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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.

Product Citations
Customer Product Validations & Biological Datas
Source Allergol Int (2015). Figure 2. GW3965
Method Western Blot
Cell Lines mice
Concentrations 1 μM
Incubation Time 1 h
Results We examined the effects of GW3965 on the IgEþAg- or LPS-induced protein expression of IL- 1a, IL-1b, IL-6, and TNF-a. Consistent with our microarray data, GW3965 significantly attenuated the protein expression of IL-1a and IL-1b, but not of IL-6 or TNF-a, in MCs stimulated by IgEþAg
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 618.51
Formula C33H31NO3ClF3.HCl
CAS Number 405911-17-3
Purity 99.46%
Solubility DMSO ≥90 mg/mL
Storage at -20°C

[1] Zhang XQ, et al. Adv Healthc Mater. Nanoparticles containing a liver X receptor agonist inhibit inflammation and atherosclerosis.

[2] Stukas S, et al. Biochim Biophys Acta. The LXR agonist GW3965 increases apoA-I protein levels in the central nervous system independent of ABCA1.

[3] Leik CE, et al. Br J Pharmacol. GW3965, a synthetic liver X receptor (LXR) agonist, reduces angiotensin II-mediated pressor responses in Sprague-Dawley rats.

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Keywords: GW3965 hydrochloride, GW3965 HCl supplier, Liver X Receptor, inhibitors

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