|3-[3-[[[2-氯-3-(三氟甲基)苯基]甲基](2,2-联苯基乙基)氨基]丙氧基]苯基乙酸盐酸盐|CsnPharm

CAS No.: 405911-17-3

GW3965 盐酸盐 Catalog No. CSN12844

Synonyms: GW 3965 (hydrochloride);GW-3965;GW-3965 HCl

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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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述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].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

动物研究

剂量

Mice: 10 mg/kg^[1] (p.o.), 40 mg/kg^[5] (p.o.); 20 mg/kg^[6] (i.p), 2 mg/kg^[7] (i.v.)

给药途径

p.o., i.p., i.v.

动物药代数据

Animal	Mice^[1]
Dose	10 mg/kg
Administration	p.o.
C_max	12.7 µg/ml
T_1/2	2 h
CL

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.6168 mL
- 8.0839 mL
- 16.1678 mL
- 5 mM
- 0.3234 mL
- 1.6168 mL
- 3.2336 mL
- 10 mM
- 0.1617 mL
- 0.8084 mL
- 1.6168 mL

技术信息

CAS号

405911-17-3

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C33H32Cl2F3NO3

运输

蓝冰

分子量

618.51

别名

GW 3965 (hydrochloride);GW-3965;GW-3965 HCl

溶解度

DMSO	50.0 mg/mL (80.8 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+30% PEG300+water	1 mg/mL	clear
PO	0.5% CMC-Na	50 mg/mL	suspension

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GW3965 盐酸盐 Catalog No. CSN12844

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