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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

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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

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

Storage condition:

desiccated

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Product Name

GW3965 hydrochloride, ≥98% (HPLC), powder

Quality Level

100

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white

solubility

DMSO: ≥20 mg/mL

originator

GlaxoSmithKline

SMILES string

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

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

InChI key

NMPUWJFHNOUNQU-UHFFFAOYSA-N

Related Categories

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

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Certificates of Analysis (COA)

Lot/Batch Number

0000544388

0000466377

0000413075

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(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

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

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

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

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

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We offer a variety of small molecule research tools, such as transcription factor modulators, inhibitors of chromatin modifying enzymes, and agonists/antagonists for target identification and validation in gene regulation research; a selection of these research tools is shown below.

Global Trade Item Number

SKU	GTIN
G6295-5MG	04061833639047
G6295-25MG	04061832954394

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