BRD 7552 |
| Catalog No.GC10233 |
PDX1 inducer
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1137359-47-7
Sample solution is provided at 25 µL, 10mM.
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BRD7552 is an inducer of pancreatic and duodenal homeobox 1 (PDX1) [1][2].
PDX1 is a member of the homeodomain-containing transcription factor family. It is a key transcription factor important for both mature β cell function and pancreas development [1]. PDX1 is a master regulatory transcription factor and required for β-cell transdifferentiation [2].
In human cells, BRD7552 upregulated the expression of PDX1 via epigenetically altering PDX1 promoter area [3]. BRD7552 was discovered as a PDX1 inducer in a cell-based phenotypic screening assay. It was used to induce the expression of PDX1. In PANC-1 cells, BRD7552 up-regulated mRNA and protein levels of PDX1. BRD7552 changed epigenetic markers within the PDX1 promoter region that was consistent with transcriptional activation. In cell culture, BRD7552 partially complemented PDX1, enhancing insulin expression induced by the introduction of three genes in PANC-1 cells [2]. In PANC-1 cells, nine-day treatment with BRD7552 dose-dependently increased insulin mRNA expression. In primary human islet cells, three of five donor samples treated with BRD7552 showed significantly dose-dependent induction of PDX1 after 3 or 5 days and of insulin after a 5-day treatment [1]. BRD7552 was capable of inducing the expression of PDX1 in the human PANC-1 ductal cell line [4].
No in vivo application data of this product had been found.
References:
[1]. Yuan Y, Hartland K, Boskovic Z, et al. A small-molecule inducer of PDX1 expression identified by high-throughput screening[J]. Chemistry & biology, 2013, 20(12): 1513-1522.
[2]. Yuan Y. Small-Molecule Modulators of Pancreatic Ductal Cells: Histone Methyltransferases and β-Cell Transdifferentiation [D]. 2013.
[3]. Zhao Y. Developing Therapies with Functional Beta Cells to Treat Diabetes[J]. International Journal of Translational Science, 2015, 1: 41-66.
[4]. Fodor A, Cozma A, Karnieli E. Personalized epigenetic management of diabetes[J]. Personalized Medicine, 2015, 12(5): 497-514.
| Cas No. | 1137359-47-7 | SDF | |
| Chemical Name | ethyl 4-(((((2R,3R,4S,5R,6S)-4,5-bis((benzo[d][1,3]dioxol-5-ylcarbamoyl)oxy)-2-(hydroxymethyl)-6-methoxytetrahydro-2H-pyran-3-yl)oxy)carbonyl)amino)benzoate | ||
| Canonical SMILES | O=C(OCC)C1=CC=C(NC(O[C@@H]2[C@@H](CO)O[C@H](OC)[C@H](OC(NC3=CC=C(OCO4)C4=C3)=O)[C@H]2OC(NC5=CC=C(OCO6)C6=C5)=O)=O)C=C1 | ||
| Formula | C33H33N3O15 | M.Wt | 711.63 |
| Solubility | ≥ 71.2mg/mL in DMSO | 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. |
||
| 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 | 1.4052 mL | 7.0261 mL | 14.0522 mL |
| 5 mM | 0.281 mL | 1.4052 mL | 2.8104 mL |
| 10 mM | 0.1405 mL | 0.7026 mL | 1.4052 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 21 reference(s) in Google Scholar.)
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