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GW3965 HCl是一種有效的,選擇性LXR激動劑,作用于hLXRα和hLXRβ,無細胞試驗中EC50分別為190和30 nM。
GW3965 HCl Chemical Structure
CAS: 405911-17-3
Skerrett R, et al. J Biol Chem. 2015 Aug 28;290(35):21591-602.
相關靶點 | LXR-α LXR-β | 點擊展開 |
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相關產品 | T0901317 LXR-623 SR9243 AZ876 | 點擊展開 |
相關化合物庫 | 代謝化合物庫 抗癌代謝化合物庫 谷氨酰胺代謝化合物庫 糖代謝化合物庫 脂代謝化合物庫 | 點擊展開 |
細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
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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 | ||
點擊查看更多細胞系數據 |
產品描述 | GW3965 HCl是一種有效的,選擇性LXR激動劑,作用于hLXRα和hLXRβ,無細胞試驗中EC50分別為190和30 nM。 | ||||||
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靶點 |
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分子量 | 618.51 | 分子式 | C33H31ClF3NO3.HCl |
CAS號 | 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 | ||
儲存條件(自收到貨起) | |||
體外溶解度 |
DMSO : 100 mg/mL ( (161.67 mM) ;DMSO吸濕會降低化合物溶解度,請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計算器 |
體內溶解度 現配現用,請按從左到右的順序依次添加,澄清后再加入下一溶劑 |
動物體內配方計算器 |
動物體內配方計算器(澄清溶液)
第一步:請輸入基本實驗信息(考慮到實驗過程中的損耗,建議多配一只動物的藥量)
第二步:請輸入動物體內配方組成(配方適用于不溶于水的藥物;不同批次藥物配方比例不同,請聯(lián)系Selleck為您提供正確的澄清溶液配方)
計算結果:
工作液濃度: mg/ml;
DMSO母液配制方法: mg 藥物溶于μL DMSO溶液(母液濃度mg/mL,注:如該濃度超過該批次藥物DMSO溶解度,請先聯(lián)系Selleck);
體內配方配制方法:取μL DMSO母液,加入μL PEG300,混勻澄清后加入μL Tween 80,混勻澄清后加入μL ddH2O,混勻澄清。
體內配方配制方法:取μL DMSO母液,加入μL Corn oil,混勻澄清。
注意:1. 首先保證母液是澄清的;
2.一定要按照順序依次將溶劑加入,進行下一步操作之前必須保證上一步操作得到的是澄清的溶液,可采用渦旋、超聲或水浴加熱等物理方法助溶。
在訂購、運輸、儲存和使用我們的產品的任何階段,您遇到的任何問題,均可以通過撥打我們的熱線電話400-668-6834,或者技術支持郵箱tech@selleck.cn,直接聯(lián)系到我們。我們會在24小時內盡快聯(lián)系您。
如果有其他問題,請給我們留言。
* 必填項
問題 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.