G6295

GW3965 hydrochloride

Name: GW3965 hydrochloride
Brand: SIGMA

≥98% (HPLC), powder, liver X receptors agonist

Synonym(s):

3-[3-[N-(2-Chloro-3-trifluoromethylbenzyl)-(2,2-diphenylethyl)amino]propyloxy]phenylacetic acid hydrochloride

Select a Size

All Photos(1)

About This Item

Empirical Formula (Hill Notation):

C₃₃H₃₁F₃ClNO₃ · HCl

CAS Number:

405911-17-3

Molecular Weight:

618.51

UNSPSC Code:

12352200

PubChem Substance ID:

24724494

NACRES:

NA.77

MDL number:

MFCD08276920

Product Name

GW3965 hydrochloride, ≥98% (HPLC), powder

SMILES string

Cl[H].OC(=O)Cc1cccc(OCCCN(CC(c2ccccc2)c3ccccc3)Cc4cccc(c4Cl)C(F)(F)F)c1

InChI key

NMPUWJFHNOUNQU-UHFFFAOYSA-N

InChI

1S/C33H31ClF3NO3.ClH/c34-32-27(15-8-17-30(32)33(35,36)37)22-38(18-9-19-41-28-16-7-10-24(20-28)21-31(39)40)23-29(25-11-3-1-4-12-25)26-13-5-2-6-14-26;/h1-8,10-17,20,29H,9,18-19,21-23H2,(H,39,40);1H

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white

solubility

DMSO: ≥20 mg/mL

originator

GlaxoSmithKline

Quality Level

100

Related Categories

Bioactive Small Molecule Agonists

Bioactive Small Molecules

Biochem/physiol Actions

GW3965 is a liver X receptor full agonist on hLXRα and hLXRβ in cell-based assays with EC₅₀ = 190 nM and 30 nM, respectively.

GW3965 is a liver X receptor full agonist on hLXRα and hLXRβ. GW3965 has an EC₅₀= 125 nM in a cell-free ligand-sensing assay of LXRα and profiles as a full agonist on hLXRα and hLXRβ in cell-based assays with EC₅₀ = 190 nM and 30 nM, respectively. It is orally active in mice. When screened against a panel of nuclear receptors, it cross-reacted with only the pregnane X receptor (PXR). The literature agonist, T0901317 (Tularik), had an EC₅₀= 60 nM and 85 nM in the cell-free and cell-based assays, respectively.

Features and Benefits

This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

pictograms

GHS05,GHS07

signalword

Danger

hcodes

H302,H318,H413

pcodes

P264 - P273 - P280 - P301 + P312 - P305 + P351 + P338 - P501

Hazard Classifications

Acute Tox. 4 Oral - Aquatic Chronic 4 - Eye Dam. 1

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

dust mask type N95 (US), Eyeshields, Gloves

Choose from one of the most recent versions:

Certificates of Analysis (COA)

Lot/Batch Number

Don't see the Right Version?

If you require a particular version, you can look up a specific certificate by the Lot or Batch number.

Search for a COA

Already Own This Product?

Find documentation for the products that you have recently purchased in the Document Library.

Visit the Document Library

Adverse outcome pathway-based analysis of liver steatosis in vitro using human liver cell lines.

Mawien Karaca et al.

STAR protocols, 4(3), 102500-102500 (2023-08-24)

Here, we present an in vitro test battery to analyze chemicals for their potential to induce liver triglyceride accumulation, a hallmark of liver steatosis. We describe steps for using HepG2 and HepaRG human hepatoma cells in conjunction with a combination of

(E)-7-Ethylidene-lithocholic Acid (7-ELCA) Is a Potent Dual Farnesoid X Receptor (FXR) Antagonist and GPBAR1 Agonist Inhibiting FXR-Induced Gene Expression in Hepatocytes and Stimulating Glucagon-like Peptide-1 Secretion From Enteroendocrine Cells.

Alzbeta Stefela et al.

Frontiers in pharmacology, 12, 713149-713149 (2021-09-07)

Bile acids (BAs) are key signaling steroidal molecules that regulate glucose, lipid, and energy homeostasis via interactions with the farnesoid X receptor (FXR) and G-protein bile acid receptor 1 (GPBAR1). Extensive medicinal chemistry modifications of the BA scaffold led to

ATF3 and CH25H regulate effector trogocytosis and anti-tumor activities of endogenous and immunotherapeutic cytotoxic T lymphocytes.

Zhen Lu et al.

Cell metabolism, 34(9), 1342-1358 (2022-09-08)

Effector trogocytosis between malignant cells and tumor-specific cytotoxic T lymphocytes (CTLs) contributes to immune evasion through antigen loss on target cells and fratricide of antigen-experienced CTLs by other CTLs. The mechanisms regulating these events in tumors remain poorly understood. Here

FOXA1 Reprogramming Dictates Retinoid X Receptor Response in ESR1-Mutant Breast Cancer.

Yang Wu et al.

Molecular cancer research : MCR, 21(6), 591-604 (2023-03-18)

Estrogen receptor alpha (ER/ESR1) mutations occur in 30% to 40% of endocrine resistant ER-positive (ER+) breast cancer. Forkhead box A1 (FOXA1) is a key pioneer factor mediating ER-chromatin interactions and endocrine response in ER+ breast cancer, but its role in

Pleiotropic effects of antitumour alkylphospholipids on cholesterol transport and metabolism.

Pablo Ríos-Marco et al.

Experimental cell research, 340(1), 81-90 (2015-12-30)

Alkylphospholipid (APL) analogs are a new class of membrane-directed synthetic compounds with a variety of biological actions and clinical applications. In particular, these agents are promising candidates in cancer treatment. We have demonstrated that after prolonged treatment APLs alter intracellular

View All Related Papers

Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.

Contact Technical Service