Home Metabolism Liver X Receptor agonist GW3965 HCl 仅限科研使用

GW3965 HCl

GW3965 HCl是一种有效的，选择性LXR激动剂，作用于hLXRα和hLXRβ，无细胞试验中EC50分别为190和30 nM。

GW3965 HCl Chemical Structure

GW3965 HCl Chemical Structure

CAS: 405911-17-3

规格 价格 库存 购买数量
10mM (1mL in DMSO) 1966.57 现货
5mg 790.51 现货
50mg 4654.57 现货
200mg 7944.3 现货
1g 27764.1 现货
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常与GW3965 HCl一起在实验中被使用的化合物

Carboplatin

在MAS98.12模型中，GW3965和Carboplatin比单独Carboplatin显着减小相对肿瘤体积。

Pioglitazone

GW3965和Pioglitazone组合预处理原代小胶质细胞可导致iNOS转录物显着减少。

Bexarotene

GW3965HCl和Bexarotene诱导急性髓系白血病(AML)细胞的分化和凋亡。

Gefitinib

GW3965可以增加Gefitinib诱导的HCC827/GR-8-2细胞系细胞凋亡和细胞周期停滞。

Navitoclax (ABT-263)

在A375异种移植模型中，GW3965和Navitoclax(ABT-263)联合治疗比单独使用任一药物更能明显抑制肿瘤生长。

GW3965 HCl相关产品

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息(PMID)
HEK293 10 uM 20 hrs Activation of rat LXRbeta expressed in HEK293 cells co-expressing human RXRalpha at 10 uM after 20 hrs by luciferase reporter gene assay 28006909
HEK293 10 uM 20 hrs Activation of human LXRalpha expressed in HEK293 cells co-expressing human RXRalpha at 10 uM after 20 hrs by luciferase reporter gene assay 28006909
HepG2 Function assay 500 nM Inhibition of 2-(3-(3-((2-chloro-3-(trifluoromethyl)benzyl)(2,2-diphenylethyl)amino)propoxy)phenyl)acetic acid-induced srebp1c mRNA expression in human HepG2 cells at 500 nM 18800767
HepG2 Function assay 500 nM Inhibition of 2-(3-(3-((2-chloro-3-(trifluoromethyl)benzyl)(2,2-diphenylethyl)amino)propoxy)phenyl)acetic acid-induced fas mRNA expression in human HepG2 cells at 500 nM 18800767
RAW264.7 Function assay 1 uM Reduction of LPS-stimulated iNOS gene expression in mouse RAW264.7 cells expressing LXRalpha at 1 uM by luciferase reporter gene assay 18800767
RAW264.7 Function assay 1 uM Inhibition of LPS-stimulated nuclear co-repressor release from iNOS promoter in mouse RAW264.7 cells at 1 uM by RT-PCR 18800767
HeLa Function assay 1 uM Induction of LXRbeta SUMOylation by SUMO2 in human HeLa cells at 1 uM by Western blot analysis 18800767
HeLa Function assay 1 uM Induction of LXRbeta SUMOylation by SUMO3 in human HeLa cells at 1 uM by Western blot analysis 18800767
HeLa Function assay 1 uM Induction of LXRalpha SUMOylation by SUMO3 in human HeLa cells at 1 uM by Western blot analysis 18800767
THP1 Antiinflammatory assay 6 hrs Antiinflammatory activity against human THP1 cells assessed as inhibition of LPS-stimulated IL6 production after 6 hrs by ELISA, IC50 = 0.02 μM. 18800767
COS7 Function assay 16 hrs Agonist activity at human LXRbeta receptor transfected in COS7 cells after 16 hrs by reporter transactivation assay, EC50 = 0.015 μM. 17587573
THP1 Function assay 18 hrs Induction of cholesterol efflux in THP1 cells after 18 hrs, EC50 = 0.01 μM. 17416521
RAW264.7 Function assay 24 hrs Induction of [3H]cholesterol efflux in mouse RAW264.7 cells loaded with acetylated-LDL after 24 hrs, EC50 = 0.029 μM. 19717304
SH-SY5Y Function assay 24 hrs 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
SH-SY5Y Function assay 24 hrs Agonist activity at human LXRalpha expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay, EC50 = 0.31 μM. 19264481
CHOK1 Function assay 24 hrs 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
CHOK1 Function assay 24 hrs Agonist activity at Gal4-tagged LXRalpha (unknown origin) expressed in CHOK1 cells after 24 hrs by luciferase reporter gene assay, EC50 = 1.3 μM. 25677664
THP1 Function assay Agonist activity at GAL-linked human LXRbeta expressed in THP1 cells assessed as stimulation of co-activator recruitment by FRET assay, EC50 = 0.027 μM. 17665897
COS7 Function assay Activation of LXRbeta co-transfected in COS7 cells with RXRalpha by reporter transactivation assay, EC50 = 0.015 μM. 17416521
THP1 Function assay Induction of cholesterol efflux in THP1 cells, EC50 = 0.01 μM. 17587573
THP1 Function assay Stimulation of [3H]cholesterol efflux in human THP1 foam cells loaded with ac-LDL, EC50 = 0.031 μM. 18973288
CV1 Function assay Antagonist activity at LXRbeta ligand binding domain assessed as inhibition of T1317-induced transcriptional activity in african green monkey CV1 cells co-transfected with Gal4-SRC1 by luciferase reporter assay, IC50 = 0.03981 μM. 20345102
THP1 Function assay Agonist activity at GAL-linked human LXRalpha expressed in THP1 cells assessed as stimulation of coactivator recruitment by FRET assay, EC50 = 0.097 μM. 17665897
CV1 Function assay Antagonist activity at LXRalpha ligand binding domain assessed as inhibition of T1317-induced transcriptional activity in african green monkey CV1 cells co-transfected with Gal4-SRC1 by luciferase reporter assay, IC50 = 0.1 μM. 20345102
HepG2 Function assay Effect on SREBP1c gene expression in human HepG2 cells, EC50 = 0.21 μM. 18973288
HuH7 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
CHO Function assay Agonist activity at human LXR beta receptor expressed in CHO cells by reporter assay, EC50 = 0.41 μM. 17034119
THP1 Function assay Effect on ABCA1 gene expression in human differentiated THP1 cells, EC50 = 0.434 μM. 18973288
CV1 Function assay Agonist activity at LXRbeta ligand binding domain-mediated transcriptional activity in african green monkey CV1 cells co-transfected with Gal4-SRC1 by luciferase reporter assay, EC50 = 0.50119 μM. 20345102
HuH7 Function assay Agonist activity at human recombinant LXRalpha ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay, EC50 = 0.66 μM. 18973288
CV1 Function assay Agonist activity at LXRalpha ligand binding domain-mediated transcriptional activity in african green monkey CV1 cells co-transfected with Gal4-SRC1 by luciferase reporter assay, EC50 = 0.79433 μM. 20345102
HepG2 Function assay Effect on triglyceride accumulation in human HepG2 cells, EC50 = 2.002 μM. 18973288
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
点击查看更多细胞系数据

生物活性

产品描述 GW3965 HCl是一种有效的，选择性LXR激动剂，作用于hLXRα和hLXRβ，无细胞试验中EC50分别为190和30 nM。
靶点
hLXRβ [1]
(Cell-free assay)		 LXRα/SRC1 LiSA [1]
(Cell-free assay)		 hLXRα [1]
(Cell-free assay)
30 nM(EC50) 125 nM(EC50) 190 nM(EC50)
体外研究(In Vitro)
体外研究活性

GW3965使类固醇受体共激活因子1聚集到LXRα，在无细胞配体检测试验中，EC50 为125 nM。[1]

GW3965对hLXRα 和 hLXRβ表现出有效的拮抗活性，在细胞试验中EC50分别为190 nM 和30 nM。此外，GW3965也对其他核受体表现出优良的选择性。[1]

在人胰岛中，GW3965 (1 μM)降低选定促炎性细胞因子，包括IL-8，单核细胞趋化蛋白-1和组织因子的表达。[4]
实验图片 检测方法 检测指标 实验图片 PMID
Western blot LXRα / LXRβ / ABCA1 / ABCG1 Skp2 / pEGFR / EGFR / pERK / ERK 11604492
Immunofluorescence pRelA LAMP-1 / LDLR 26635040
Growth inhibition assay Cell viability 25184494
体内研究(In Vivo)
体内研究活性

在小鼠体内，GW3965在10 mg/kg剂量下使ABCA1表达上调8倍，并使循环水平提高30%，Cmax为12.7 μg/mL ，t1/2为2小时。[1]

在LDLR−/−和apoE−/−小鼠体内，GW3965 (10mg/kg)诱导ABCA1 和ABCG1表达，并表现出有效的抗动脉粥样硬化活性。[2]

在雄性sprague-dawley大鼠体内，GW3965降低Ang II介导的血压增加，并减少血管Ang II受体基因表达。[3]

在恶性胶质瘤小鼠模型中，GW3965导致LDLR降解，增加ABCA1胆固醇外排转运体的表达，从而有效促进肿瘤细胞死亡。[5]
动物实验 Animal Models C57BL/6 小鼠
Dosages ≤10 mg/kg
Administration 口服
  • https://pubmed.ncbi.nlm.nih.gov/11985463/
  • https://pubmed.ncbi.nlm.nih.gov/12032330/
  • https://pubmed.ncbi.nlm.nih.gov/17420776/
  • https://pubmed.ncbi.nlm.nih.gov/19415233/
  • https://pubmed.ncbi.nlm.nih.gov/22059152/
  • https://pubmed.ncbi.nlm.nih.gov/34686867/

化学信息&溶解度

分子量 618.51 分子式

C33H31ClF3NO3.HCl
CAS号 405911-17-3 SDF Download GW3965 HCl SDF
Smiles C1=CC=C(C=C1)C(CN(CCCOC2=CC=CC(=C2)CC(=O)O)CC3=C(C(=CC=C3)C(F)(F)F)Cl)C4=CC=CC=C4.Cl
储存条件(自收到货起)

体外溶解度
批次：

DMSO : 100 mg/mL ( (161.67 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解配方
批次：

现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂

 动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

mg/kg g μL 只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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常见问题及建议解决方法

问题 1:
How to formulate the compound for mouse in vivo experiment?

回答：
S2630 GW3965 HCl can be dissolved in 2% DMSO/30% PEG 300/dd H2O at 10 mg/mL as a homogeneous suspension. This vehicle is suitable for oral gavage to mice.

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