GW3965 HCl is a selective and non-steroidal LXR agonist with EC50 values of 190 and 30 nM for hLXRα and hLXRβ, respectively.
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LXRs (Liver X receptors) are ligand-activated transcription factors of the nuclear receptor superfamily, consist of two LXR isoforms termed alpha and beta. It is characterized as key transcriptional regulators of lipid and carbohydrate metabolism. GW3965 is a potent and selective tertiary-amine-derived nonsteroidal LXR agonist with EC50 values of 190 and 30 nM for LXRα and LXRβ (measured by LXRα cell-based reporter gene assay), respectively. It could recruit the steroid receptor coactivator 1 to human LXRα in a cell-free ligand-sensing assay with an EC50 of 125 nM. A single dose of GW3965 at dose of 10mg/kg achieved oral bioavailability of 70% at 2h post treatment in mice. The pharmacological activity could be evaluated in mce by dosing at 10 mg/kg bid for 14 days, as the expression of reverse cholesterol transporter ABCA1, a target gene of LXR, was increased 8-fold in the small intestine and 7-fold in peripheral macrophages by day 3, while plasma levels of HDLc increased 30% at day 3 and was maintained until day 14[1]. Through activation of GW3965, GW3965 affected pathways of glucose and lipid metabolism. It altered fat tissue distribution in ob/ob female mice[2]. GW3965 exhibited potent antiatherogenic activity in both two models, LDLR-/- mice and apoE-/- mice, as reducing lesion area by 34%-53%[3]. As LXRs and their ligands are negative regulators of macrophage inflammatory gene expression, treatment with GW3965 could reduce inflammation in a model of irritant contact dermatitis[4] and alter adipose tissue inflammation in ob/ob female mice[2].
GW3965 hydrochloride 细胞研究
细胞系
浓度
检测类型
检测时间
活动说明
数据源
CHO cells
Function assay
Agonist activity at human LXR beta receptor expressed in CHO cells by reporter assay, EC50=0.41 μM
17034119
CHOK1 cells
Function assay
24 h
Agonist activity at Gal4-tagged LXRbeta (unknown origin) expressed in CHOK1 cells after 24 hrs by luciferase reporter gene assay, EC50=0.42 μM
25677664
COS7 cells
Function assay
Activation of LXRbeta co-transfected in COS7 cells with RXRalpha by reporter transactivation assay, EC50=0.015 μM
17416521
human HeLa cells
1 μM
Function assay
Induction of LXRbeta SUMOylation by SUMO2 in human HeLa cells at 1 uM by Western blot analysis
Agonist activity at human LXR beta receptor expressed in CHO cells by reporter assay, EC50=0.41 μM
17034119
CHOK1 cells
Function assay
24 h
Agonist activity at Gal4-tagged LXRbeta (unknown origin) expressed in CHOK1 cells after 24 hrs by luciferase reporter gene assay, EC50=0.42 μM
25677664
COS7 cells
Function assay
Activation of LXRbeta co-transfected in COS7 cells with RXRalpha by reporter transactivation assay, EC50=0.015 μM
17416521
human HeLa cells
1 μM
Function assay
Induction of LXRbeta SUMOylation by SUMO2 in human HeLa cells at 1 uM by Western blot analysis
18800767
human HepG2 cells
Function assay
Effect on SREBP1c gene expression in human HepG2 cells, EC50=0.21 μM
18973288
human HuH7 cells
Function assay
Agonist activity at human recombinant LXRbeta ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay, EC50=0.31 μM
18973288
human primary hepatocytes
1 μM
Function assay
Induction on FAS gene expression in human primary hepatocytes at 1 uM
17665897
human SH-SY5Y cells
Function assay
24 h
Agonist activity at human LXRbeta expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay, EC50=0.13 μM
19264481
human THP1 cells
Function assay
6 h
Antiinflammatory activity against human THP1 cells assessed as inhibition of LPS-stimulated IL6 production after 6 hrs by ELISA, IC50=0.02 μM
18800767
mouse RAW264.7 cells
Function assay
24 h
Induction of [3H]cholesterol efflux in mouse RAW264.7 cells loaded with acetylated-LDL after 24 hrs, EC50=0.029 μM
19717304
THP1 cells
Function assay
18 h
Induction of cholesterol efflux in THP1 cells after 18 hrs, EC50=0.01 μM
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