GW3965 hydrochloride | GW 3965 (hydrochloride);GW3965 HCl | LXR

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GW3965 hydrochloride {[allProObj[0].p_purity_real_show]}

货号：A150197 同义名： GW 3965 (hydrochloride);GW3965 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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GW3965 hydrochloride 化学结构
CAS号：405911-17-3

GW3965 hydrochloride 3D分子结构
CAS号：405911-17-3

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GW3965 hydrochloride 纯度/质量文件产品仅供科研

货号：A150197 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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GW3965 hydrochloride 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].

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	18800767

GW3965 hydrochloride 动物研究

Dose

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.)

Administration

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

Pharmacokinetics

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

GW3965 hydrochloride 参考文献

[1]Collins JL, Fivush AM, et al. Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines. J Med Chem. 2002 May 9;45(10):1963-6.

[2]Archer A, Stolarczyk E, et al. LXR activation by GW3965 alters fat tissue distribution and adipose tissue inflammation in ob/ob female mice. J Lipid Res. 2013 May;54(5):1300-11.

[3]Joseph SB, McKilligin E, et al. Synthetic LXR ligand inhibits the development of atherosclerosis in mice. Proc Natl Acad Sci U S A. 2002 May 28;99(11):7604-9.

[4]Joseph SB, Castrillo A, et al. Reciprocal regulation of inflammation and lipid metabolism by liver X receptors. Nat Med. 2003 Feb;9(2):213-9. Epub 2003 Jan 13.

[5]Guo D, Reinitz F, et al. An LXR agonist promotes glioblastoma cell death through inhibition of an EGFR/AKT/SREBP-1/LDLR-dependent pathway. Cancer Discov. 2011 Oct;1(5):442-56.

[6]He Q, Pu J, et al. Liver X receptor agonist treatment attenuates cardiac dysfunction in type 2 diabetic db/db mice. Cardiovasc Diabetol. 2014 Nov 22;13:149.

[7]Spyridon M, Moraes LA, et al. LXR as a novel antithrombotic target. Blood. 2011 May 26;117(21):5751-61.

GW3965 hydrochloride 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.62mL

0.32mL

0.16mL

8.08mL

1.62mL

0.81mL

16.17mL

3.23mL

1.62mL

GW3965 hydrochloride 技术信息

CAS号	405911-17-3
分子式	C₃₃H₃₂Cl₂F₃NO₃
分子量	618.513

别名	GW 3965 (hydrochloride);GW3965 HCl
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature

溶解度

DMSO: 105 mg/mL(169.76 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

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

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	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	17416521

GW3965 hydrochloride {[allProObj[0].p_purity_real_show]}

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GW3965 hydrochloride 质控信息

GW3965 hydrochloride 生物活性

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GW3965 hydrochloride 动物研究

GW3965 hydrochloride 参考文献

GW3965 hydrochloride 实验方案

GW3965 hydrochloride 技术信息

最近浏览的产品

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摩尔计算器

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总药量计算器

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