BIM5078 |
| Catalog No.GC13937 |
HNF4α antagonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 337506-43-1
Sample solution is provided at 25 µL, 10mM.
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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 | |
| Chemical Name | 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 | ||
| Formula | C14H10ClN3O4S | M.Wt | 351.8 |
| Solubility | ≤5mg/ml in DMSO;3mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)
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