2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. LXR
  4. SR9238

SR9238 是一种合成的肝 X 受体 (LXR) 反向激动剂，对于 LXRα 和 LXRβ 的 IC50 值分别为 214 nM 和 43 nM。

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SR9238 Chemical Structure

SR9238 Chemical Structure

CAS No. : 1416153-62-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1009
In-stock
5 mg ￥770
In-stock
10 mg ￥1350
In-stock
25 mg ￥2900
In-stock
50 mg ￥4212
In-stock
100 mg ￥5896
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

SR9238 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

SR9238 is a synthetic liver X receptor (LXR) inverse agonist with IC50s of 214 nM and 43 nM for LXRα and LXRβ, respectively.

IC50 & Target

IC50: 43 nM (LXRβ), 214 nM (LXRα)[1]
体外研究
(In Vitro)

Results from the cell-based cotransfection assays demonstrate that SR9238 is a synthetic LXR inverse agonist with IC50s of 214 nM and 43 nM for LXRα and LXRβ, respectively. SR9238 also effectively suppresses transcription from a fatty acid synthase (Fasn) promoter driven luciferase reporter. It is found that SR9238 induces increased interaction of CoRNR box peptides derived from NCoR (NCoR ID1 and NCoR ID2) with both LXRα and LXRβ, while causing decreased interaction with a coactivator NR box peptide derived from TRAP220. SR9238-induced recruitment of CoRNR box peptides is dose-dependent for both LXRα and LXRβ. HepG2 cells treated with SR9238 result in a significant decrease in Fasn and Srebp1c mRNA expression[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

SR9238 相关抗体:
体内研究
(In Vivo)

Approximately 6 μM SR9238 is detected in the liver 2h after the injection of SR9238, but no compound is detected in the plasma. SR9238 is also detected in the intestine with either ip or oral administration. SR9238-treated mice display greatly reduced lipid content in the liver. Results demonstrate that both Tnfa and Il1b expression are substantially reduced (~80% and >95%, respectively) in the SR9238-treated mice when compare to the vehicle-treated mice. SR9238-treated DIO mice display considerably lower intensity of F4/80 staining versus vehicle-treated DIO mice consistent with a beneficial effect of SR9238 on non-alcoholic steatohepatitis (NASH). SR9238 treatment does not alter body weight or percent body fat composition relative to vehicle treated animals during the experiment. Treatment with SR9238 suppresses diet-induced hepatosteatosis, hepatic inflammation, and hepatocellular injury[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

595.73

Formula

C31H33NO7S2
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 50 mg/mL (83.93 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6786 mL 8.3931 mL 16.7861 mL
5 mM 0.3357 mL 1.6786 mL 3.3572 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

In Vivo:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (4.20 mM); 悬浊液; 超声助溶

    此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.20 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.87%

COA (203 KB) LCMS (271 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[1]

HepG2 cells are seeded at 5×105 cells/mL in a 4-chamber culture slide. The following day the media is removed and replaced with antibiotic-free media containing 10 μM of DMSO or SR9238 and cells are allowed to grow for 48 h. Cells are washed in TBS, fixed and fluorescently stained for SREBP2 according to the assay protocol[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Twenty-one-week-old male C57BL6 DIO mice are used. Animals are individually housed and fed a high fat diet (60% kcal/fat diet, 20% carbohydrate) for the duration of the experiment that includes SR9238 administration for 30 days (30 mg/kg, qd, ip). Prior to initiation of the experiment, animals are provided the high fat diet for 10-weeks. Animals are acclimated to the environment for one week and sham dosed with vehicle for 3 days prior to SR9238 administration. Body weight and food intake are monitored daily. Pre- and post-experiment body composition analysis is performed on all the mice. Blood is collected by cardiac puncture and used for plasma cholesterol and triglyceride measurements. Livers are weighed and immediately flash-frozen in liquid nitrogen for gene expression analysis or put in formalin on ice for histology[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

SR9238 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6786 mL 8.3931 mL 16.7861 mL 41.9653 mL
5 mM 0.3357 mL 1.6786 mL 3.3572 mL 8.3931 mL
10 mM 0.1679 mL 0.8393 mL 1.6786 mL 4.1965 mL
15 mM 0.1119 mL 0.5595 mL 1.1191 mL 2.7977 mL
20 mM 0.0839 mL 0.4197 mL 0.8393 mL 2.0983 mL
25 mM 0.0671 mL 0.3357 mL 0.6714 mL 1.6786 mL
30 mM 0.0560 mL 0.2798 mL 0.5595 mL 1.3988 mL
40 mM 0.0420 mL 0.2098 mL 0.4197 mL 1.0491 mL
50 mM 0.0336 mL 0.1679 mL 0.3357 mL 0.8393 mL
60 mM 0.0280 mL 0.1399 mL 0.2798 mL 0.6994 mL
80 mM 0.0210 mL 0.1049 mL 0.2098 mL 0.5246 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SR92381416153-62-2SR 9238SR-9238LXRLiver X receptorInhibitorinhibitorinhibit

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