BIM5078
目录号 : GC13937An HNF4α antagonist
Cas No.:337506-43-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
EC50: 11.9 nM for HNF4α
BIM5078 is a HNF4α antagonist.
Hepatocyte nuclear factor (HNF)4α is a key regulator of gene expression in cell types playing a important role in metabolic homeostasis, such as hepatocytes, enterocytes, as well as pancreatic β cells.
In vitro: The EC50 of BIM5078 was calculated to be 11.9 nM and further analyses of the data using the Hill equation showed that the Hill coefficient for BIM5078 was 0.9, consistent with a single binding complex between BIM5078 and HNF4α. In docking study, the high GoldScore indicated that it was reasonable for BIM5078 to bind in the LBP in a position similar to that of the putative endogenous ligand. Moreover, BIM5078 could potently repress HNF4α expression in T6PNE, the murine insulinoma cell line MIN6, and in the HepG2 hepatoma line, which had exceptionally high levels of HNF4α expression [1].
In vivo: BI6015, a analog of BIM5078, could induce a loss of HNF4α protein in the liver, but not in the intestine or kidney, which was consistent with the in vitro effects of BIM5078 on HNF4α expression both in human- and murine-derived cell lines. In addition, no difference in the cell number expressing the proliferation marker Ki67 was observed in liver, intestine, or kidney with BI6015, when compared with vehicle-treated animals [1].
Clinical trial: Up to now, BIM5078 is still in the preclinical development stage.
Reference:
[1] A. Kiselyuk, S. H. Lee, S. Farber-Katz, et al. HNF4α antagonists discovered by a high-throughput screen for modulators of the human insulin promoter. Chemistry & Biology 19, 806-818 (2012).
| Cas No. | 337506-43-1 | SDF | |
| 化学名 | 1-[(2-chloro-5-nitrophenyl)sulfonyl]-2-methyl-1H-benzimidazole | ||
| Canonical SMILES | CC1=NC2=CC=CC=C2N1S(C3=C(Cl)C=CC([N+]([O-])=O)=C3)(=O)=O | ||
| 分子式 | C14H10ClN3O4S | 分子量 | 351.8 |
| 溶解度 | ≤5mg/ml in DMSO;3mg/ml in dimethyl formamide | 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 | 2.8425 mL | 14.2126 mL | 28.4252 mL |
| 5 mM | 0.5685 mL | 2.8425 mL | 5.685 mL |
| 10 mM | 0.2843 mL | 1.4213 mL | 2.8425 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。