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G6295

GW3965 hydrochloride

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

Synonyme(s) :

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

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A propos de cet article

Formule empirique (notation de Hill) :
C33H31F3ClNO3 · HCl
Numéro CAS:
405911-17-3
Poids moléculaire :
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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Nom du produit

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

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

CorrosionExclamation mark
GHS05,GHS07

signalword

Danger

Hazard Classifications

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

Classe de stockage

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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Certificats d'analyse (COA)

Lot/Batch Number
0000544388
0000544388
0000466377
0000413075
0000413075

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Consulter la Bibliothèque de documents

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
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
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
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