首页工具

购物车

GW3965 hydrochloride

产品编号 T6310 CAS 405911-17-3

别名: GW3965 HCl

GW3965 hydrochloride (GW3965 HCl) 是一种肝 X 受体 (LXR) 激动剂，主要作用于 hLXRα (EC50:190 nM) 和 hLXRβ (EC50:30 nM)

TargetMol的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

GW3965 hydrochloride, CAS 405911-17-3

规格	价格/CNY	货期
1 mg	￥ 228	现货
2 mg	￥ 329	现货
5 mg	￥ 578	现货
10 mg	￥ 828	现货
25 mg	￥ 1,680	现货
50 mg	￥ 3,230	现货
100 mg	￥ 4,780	现货
500 mg	￥ 9,870	待询
1 mL * 10 mM (in DMSO)	￥ 789	现货

大包装超大折扣，点击咨询

其他形式的 GW3965 hydrochloride:

GW3965
询价

选择批次

纯度: 99.75%

纯度: 99.51%

更多批次查询请联系客服

生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	GW3965 hydrochloride (GW3965 HCl) is an effective and specific LXR agonist for hLXRα/β (EC50: 190/30 nM).
靶点活性	LXRα (human):190 nM(EC50), LXRβ (human):30 nM(EC50)
体外活性	GW3965 recruits the steroid receptor coactivator 1 to human LXRα with EC50 of 125 nM in a cell-free ligand-sensing assay. [1] GW3965 shows a potent antagonistic activity against hLXRα and hLXRβ in cell-based assays with EC50 of 190 nM and 30 nM, respectively. Besides, GW3965 also sows excellent selectivity over other nuclear receptors. [1] In human islets, GW3965 (1 μM) reduces expression of selected pro-inflammatory cytokines including IL-8, monocyte chemotactic protein-1 and tissue factor. [4]
体内活性	In mice, GW3965 at a dose of 10 mg/kg upregulates ABCA1 expression 8-fold and raises circulating levels of HDL by 30% with Cmax of 12.7 μg/mL and t1/2 of 2 hours. [1] GW3965 (10 mg/kg) induces expression of ABCA1 and ABCG1 and shows potent antiatherogenic activity in both LDLR?/? and apoE?/? mice. [2] In male sprague-dawley rats, GW3965 reduces Ang II-mediated increases in blood pressure and decreases vascular Ang II receptor gene expression. [3] In Glioblastoma mouse model, GW3965 results in inducible degrader of LDLR-mediated LDLR degradation, increased expression of the ABCA1 cholesterol efflux transporter, and thus potently promotes tumor cell death. [5]
激酶实验	Steady-state drug accumulation assay: AuxB1 and CHrB30 cells are grown to confluency in 12-well (24 mm) tissue culture dishes and the steady-state accumulation of [3H]-vinblastine is measured. Accumulation is initiated by the addition of 0.1 μ Ci [3H]-vinblastine and unlabelled vinblastine to a final concentration of 100 nM . The accumulation of [3H]-paclitaxel is measured using 0.1 μ Ci [3H]-paclitaxel and unlabelled drug to a final concentration of 1 μM . Cells are incubated in a reaction volume of 1 mL for 60 min at 37 ℃ under 5% CO2 in order to reach steady-state. The effect of the modulators XR9576 on [3H]-ligand accumulation is investigated in the concentration range 10-9 - 10-6 M. Modulators are added from a DMSO stock giving a final solvent concentration of 0.2 % (v/v). Following cell harvesting, accumulated drug is measured by liquid scintillation counting and normalized for cell protein content. Plots of amount accumulated as a function of modulator concentration are fitted with the general dose-response equation: Y={(a-b)/(1+(X/c)d)}+b Where: Y=response; a=initial response; b=final response; c=EC50 concentration; d=slope value; X=drug concentration.
细胞实验	Cells are seeded in 96 wells and are treated after 24 hours with different drugs indicated in each experiment in medium containing 1% FBS or lipoprotein deficient serum. Relative proliferation is determined using Cell Proliferation Assay Kit. Cells are incubated 1.5 hrs after adding tetrazolium salt WST-1 [2-(4-iodophenyl)-3- (4-nitrophenyl)-5-(2, 4-disulfo-phenyl)-2H-tetrazolium, monosodium salt] at 5% CO2, 37oC and the absorbance of the treated and untreated cells are measured using a microplate reader at 420 to 480 nm. Cells seeded in 12 well plates are counted using a hemocytometer, and dead cells are assessed using trypan blue exclusion assays.

别名	GW3965 HCl
分子量	618.51
分子式	C33H31ClF3NO3·HCl
CAS No.	405911-17-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 61.9 mg/mL (100 mM)

Ethanol: 12.4 mg/mL (20 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO / Ethanol	1 mM	1.6168 mL	8.0839 mL	16.1679 mL	40.4197 mL
	5 mM	0.3234 mL	1.6168 mL	3.2336 mL	8.0839 mL
	10 mM	0.1617 mL	0.8084 mL	1.6168 mL	4.042 mL
	20 mM	0.0808 mL	0.4042 mL	0.8084 mL	2.021 mL
DMSO	50 mM	0.0323 mL	0.1617 mL	0.3234 mL	0.8084 mL
DMSO	100 mM	0.0162 mL	0.0808 mL	0.1617 mL	0.4042 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Collins JL, et al. J Med Chem. 2002, 45(10), 1963-1966. 2. Joseph SB, et al. Proc Natl Acad Sci U S A. 2002, 99(11), 7604-7609. 3. Leik CE, et al. Br J Pharmacol. 2007, 151(4), 450-456. 4. Scholz H, et al. Diabetologia. 2009, 52(7), 1352-1362. 5. Guo D, et al. Cancer Discov. 2011, 1(5), 442-456.

文献引用

1. Liu Y, Wang Z, Jin H, et al.Squalene-epoxidase-catalyzed 24 (S), 25-epoxycholesterol synthesis promotes trained-immunity-mediated antitumor activity.Cell Reports.2024, 43(4).

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

GW3965 hydrochloride 405911-17-3 Metabolism Liver X Receptor GW-3965 GW3965 HCl Liver X receptor GW-3965 hydrochloride Inhibitor GW3965 inhibit GW3965 Hydrochloride LXR GW-3965 Hydrochloride GW 3965 GW 3965 Hydrochloride inhibitor

我们的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

沪公网安备 31010602006700号

陶术

生物

TargetMol^®中国区唯一合作伙伴

点击进入陶术生物官网

联系我们

电话：

400-820-0310

邮箱：

service@tsbiochem.com

QQ：

2881945090（终端用户）

2885109491（经销商）

经销：

终端：

地址：

上海市静安区江场三路238号8楼

GW3965 hydrochloride

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords