Free shipping on all orders over $ 500

GW3965 hydrochloride

Cat. No. M1929
GW3965 hydrochloride Structure
Synonym:

GW3965 HCl

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
2mg USD 42  USD42 In stock
5mg USD 72  USD72 In stock
10mg USD 102  USD102 In stock
50mg USD 420  USD420 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

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.

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
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 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
References

[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.

Related Liver X Receptor Products
RGX-104 hydrochloride

RGX-104 hydrochloride is a small-molecule LXR (liver X receptor) agonist that modulates innate immunity via transcriptional activation of the ApoE gene.

Iristectorigenin B

Iristectorigenin B is a liver X receptor (LXR) modulator, which stimulates the transcriptional activity of both LXR-α and LXR-β.

RGX-104

RGX-104, also known as SB 742881, is a liver X receptor beta (LXR) agonist with potential immunomodulating and antineoplastic activities.

Yamogenin

Yamogenin (Diosgenin) antagonizes the activation of the liver X receptor (LXR) in luciferase ligand assay.

SR9238

SR9238 is a liver X receptor (LXR) inverse agonist with IC50s of 214 nM and 43 nM for LXRα and LXRβ, respectively.

  Catalog
Abmole Inhibitor Catalog 2017




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

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.