GSK2033
目录号 : GC31331
An antagonist of LXRα and LXRβ
Cas No.:1221277-90-2
Sample solution is provided at 25 µL, 10mM.
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GSK2033 is an antagonist of liver X receptor α (LXRα) and LXRβ (IC50s = 0.1 and 0.398 ?M, respectively) that has no agonist activity in an LXR transactivation assay.1 It inhibits LXR agonist-induced and basal expression of the LXR target genes ATP-binding cassette transporter 1 (ABCA1) and sterol regulatory element binding protein 1c (SREBP-1c) in THP-1 and HepG2 cells, respectively. However, GSK2033 binds promiscuously to a variety of nuclear receptors including RORγ, RXRα, ERα, and ERβ in a nuclear receptor specificity assay in HEK293 cells and, in a mouse model of non-alcoholic fatty liver disease (NAFLD), it induces the expression of fatty acid synthase and SREBP-1.2
1.Zuercher, W.J., Buckholz, R.G., Campobasso, N., et al.Discovery of tertiary sulfonamides as potent liver X receptor antagonistsJ. Med. Chem.53(8)3412-3416(2010) 2.Griffett, K., and Burris, T.P.Promiscuous activity of the LXR antagonist GSK2033 in a mouse model of fatty liver diseaseBiochem. Biophys. Res. Commun.479(3)424-428(2016)
Cell experiment: | HepG2 cells are maintained in minimal essential medium supplemented with 10% FBS and antibiotics. HepG2 cells are then treated for 24 h with GSK2033 followed by assessment of expression of genes by qPCR[2]. |
Animal experiment: | 21-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 GSK2033 administration for 28 days (30 mg/kg, q. d, i. p.). Body weight and food intake are monitored daily[2]. |
References: [1]. Zuercher WJ, et al. Discovery of tertiary sulfonamides as potent liver X receptor antagonists. J Med Chem. 2010 Apr 22;53(8):3412-6. | |
| Cas No. | 1221277-90-2 | SDF | |
| Canonical SMILES | O=S(C1=C(C)C=C(C)C=C1C)(N(CC2=CC=C(C3=CC=CC(S(=O)(C)=O)=C3)C=C2)CC4=CC=C(C(F)(F)F)O4)=O | ||
| 分子式 | C29H28F3NO5S2 | 分子量 | 591.66 |
| 溶解度 | DMSO : 30 mg/mL (50.70 mM) | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6902 mL | 8.4508 mL | 16.9016 mL |
| 5 mM | 0.338 mL | 1.6902 mL | 3.3803 mL |
| 10 mM | 0.169 mL | 0.8451 mL | 1.6902 mL |
| 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） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 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GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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，
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 saline，混匀澄清。
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet