GW3965 HCl

目錄號：S2630 Purity: 99.88%

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

規(guī)格	價格	庫存
10mM (1mL in DMSO)	1966.57	現(xiàn)貨
5mg	790.51	現(xiàn)貨
50mg	4654.57	現(xiàn)貨
200mg	7944.3	現(xiàn)貨
1g	27764.1	現(xiàn)貨
更大包裝有超大折扣
400-668-6834 [email protected]

產(chǎn)品質控

批次：純度： 99.88%

99.88

常與GW3965 HCl一起在實驗中被使用的化合物

Carboplatin

在MAS98.12模型中，GW3965和Carboplatin比單獨Carboplatin顯著減小相對腫瘤體積。

Pioglitazone

GW3965和Pioglitazone組合預處理原代小膠質細胞可導致iNOS轉錄物顯著減少。

Bexarotene

GW3965HCl和Bexarotene誘導急性髓系白血病(AML)細胞的分化和凋亡。

Gefitinib (ZD1839)

GW3965可以增加Gefitinib誘導的HCC827/GR-8-2細胞系細胞凋亡和細胞周期停滯。

Navitoclax (ABT-263)

在A375異種移植模型中，GW3965和Navitoclax(ABT-263)聯(lián)合治療比單獨使用任一藥物更能明顯抑制腫瘤生長。

GW3965 HCl相關產(chǎn)品

相關靶點	LXR-α LXR-β	點擊展開
相關產(chǎn)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

細胞實驗數(shù)據(jù)示例

細胞系	實驗類型	給藥濃度	孵育時間	活性描述	文獻信息(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
點擊查看更多細胞系數(shù)據(jù)

生物活性

產(chǎn)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。

靶點

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)

體外研究(In Vitro)
體外研究活性	GW3965使類固醇受體共激活因子1聚集到LXRα，在無細胞配體檢測試驗中，EC50 為125 nM。^[1] GW3965對hLXRα 和 hLXRβ表現(xiàn)出有效的拮抗活性，在細胞試驗中EC50分別為190 nM 和30 nM。此外，GW3965也對其他核受體表現(xiàn)出優(yōu)良的選擇性。^[1] 在人胰島中，GW3965 (1 μM)降低選定促炎性細胞因子，包括IL-8，單核細胞趨化蛋白-1和組織因子的表達。^[4]
實驗圖片	檢測方法	檢測指標	實驗圖片	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

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	在小鼠體內(nèi)，GW3965在10 mg/kg劑量下使ABCA1表達上調(diào)8倍，并使循環(huán)水平提高30%，C_max為12.7 μg/mL ，t_1/2為2小時。^[1] 在LDLR−/−和apoE−/−小鼠體內(nèi)，GW3965 (10mg/kg)誘導ABCA1 和ABCG1表達，并表現(xiàn)出有效的抗動脈粥樣硬化活性。^[2] 在雄性sprague-dawley大鼠體內(nèi)，GW3965降低Ang II介導的血壓增加，并減少血管Ang II受體基因表達。^[3] 在惡性膠質瘤小鼠模型中，GW3965導致LDLR降解，增加ABCA1膽固醇外排轉運體的表達，從而有效促進腫瘤細胞死亡。^[5]
動物實驗	Animal Models	C57BL/6 小鼠
	Dosages	≤10 mg/kg
	Administration	口服

參考文獻
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/ + 展開

參考文獻

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/

+ 展開

化學信息&溶解度

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)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

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

DMSO : 50 mg/mL ( (80.83 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 33 mg/mL ( (53.35 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(nèi)溶解配方批次：現(xiàn)配現(xiàn)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(nèi)配方計算器
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產(chǎn)品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O 該配方已經(jīng)過Selleck實驗室實測。如果上述溶解方案不能滿足您的需求，可聯(lián)系Selleck銷售提供定制化測試。	5.000mg/ml (8.08mM)	以 1 mL 工作液為例,取50μL100mg/ml的澄清DMSO儲備液加到400μLPEG300中,混合均勻使其澄清;向上述體系中加入50μLTween80,混合均勻使其澄清;然后繼續(xù)加入500μLddH2O定容至1mL。工作液請現(xiàn)配現(xiàn)用!
澄清溶液	5% DMSO 1 95% Corn oil 該配方已經(jīng)過Selleck實驗室實測。如果上述溶解方案不能滿足您的需求，可聯(lián)系Selleck銷售提供定制化測試。	0.600mg/ml (0.97mM)	以1 mL工作液為例，取50μL 12mg/ml的澄清DMSO儲備液加到950μL玉米油中，混合均勻。工作液請現(xiàn)配現(xiàn)用！
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產(chǎn)品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產(chǎn)品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O 該配方已經(jīng)過Selleck實驗室實測。如果上述溶解方案不能滿足您的需求，可聯(lián)系Selleck銷售提供定制化測試。	0.800mg/ml (1.29mM)	以 1 mL 工作液為例，取50μL16mg/ml的澄清DMSO儲備液加到400μL PEG300中，混合均勻使其澄清；向上述體系中加入50μLTween80，混合均勻使其澄清；然后繼續(xù)加入500μL ddH2O定容至 1 mL。工作液請現(xiàn)配現(xiàn)用！

實驗計算

摩爾濃度計算器

質量	濃度	體積	分子量
=	×	×

稀釋計算器分子量計算器

動物體內(nèi)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）

給藥劑量 mg/kg 動物平均體重 g 每只動物給藥體積 μL 動物數(shù)量只

第二步：請輸入動物體內(nèi)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）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

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(nèi)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(nèi)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。

技術支持

在訂購、運輸、儲存和使用我們的產(chǎn)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[email protected]，直接聯(lián)系到我們。我們會在24小時內(nèi)盡快聯(lián)系您。

操作手冊

如果有其他問題，請給我們留言。

* 必填項

常見問題及建議解決方法

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.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):