YL0441
Based on 1 Customer Validation
YL0441 is an inhibitor of ΔFOSB/JUND heterodimers and ΔFOSB homomultimers, with IC50 values of 13.7 μM and 12.3 μM, respectively. YL0441 blocks the binding of ΔFOSB to DNA. YL0441 reduces ΔFOSB bound to genomic DNA in the hippocampal tissues of APP mice. YL0441 is applicable to the research of Alzheimer's disease.
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- Purity: 98.94%
- 화학식: C19H15NO6S
- 분자량:385.39
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보관:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
All AP-1 Isoforms
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Biological Activity
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ΔFOSB/JUND 13.7 |
ΔFOSB 12.3 μM (IC50) |
YL0441 (0-200 μM; 15 min) disrupts the binding of purified full-length mouse ΔFOSB/JUND heterodimers and ΔFOSB/ΔFOSB homomers to a TAMRA-labeled AP-1 consensus oligonucleotide with IC50 values of 13.7 μM and 12.3 μM, respectively[1].
YL0441 (12.5-50 μM; 72 h) shows no detectable toxicity to Neuro 2A cells at concentrations up to 50 μM after 72 h of incubation[1].
YL0441 (1 μM; up to 60 min) exhibits high metabolic stability in mouse liver microsomes, with a half-life greater than 186.38 min[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
hippocampus; for 3 consecutive days) reduces the binding level of ΔFOSB to genomic DNA in the hippocampus of APP transgenic mice by ~94%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:J20 (2-3 month-old; heterozygous transgenic; male and female; Alzheimer's disease model expressing human amyloid precursor protein with Swedish and Indiana mutations)[1]
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Dosage:50 μM; 18.5 ng per hour
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Administration:infused into the
hippocampus; continuous; 3 consecutive days -
Result:Reduced total ΔFOSB-bound genomic DNA peaks from 9642 to 540, representing a ~94% reduction in total binding events.
Decreased average peak width of remaining ΔFOSB-bound sites from ~286 bp to ~254 bp.
Reduced ΔFOSB binding to unique target genes by ~94%, with a 95% reduction in promoter-bound genes and 91% reduction in distal intergenic-bound genes.
Eliminated ΔFOSB occupancy across all genomic regions (promoters, exons, introns, distal intergenic regions), with no induction of ΔFOSB binding to novel ectopic sites.
Chemical Information
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Appearance Solid
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분자량 385.39
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화학식 C19H15NO6S
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Color Light yellow to yellow
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SMILES
O=C(/C=C/C1=CC=CO1)NC(C=C2S(O)(=O)=O)=CC=C2OC3=CC=CC=C3
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
용액&용해도
DMSO : 100 mg/mL (259.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.49 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.49 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5948 mL | 12.9739 mL | 25.9477 mL | 64.8694 mL |
| 5 mM | 0.5190 mL | 2.5948 mL | 5.1895 mL | 12.9739 mL | |
| 10 mM | 0.2595 mL | 1.2974 mL | 2.5948 mL | 6.4869 mL | |
| 15 mM | 0.1730 mL | 0.8649 mL | 1.7298 mL | 4.3246 mL | |
| 20 mM | 0.1297 mL | 0.6487 mL | 1.2974 mL | 3.2435 mL | |
| 25 mM | 0.1038 mL | 0.5190 mL | 1.0379 mL | 2.5948 mL | |
| 30 mM | 0.0865 mL | 0.4325 mL | 0.8649 mL | 2.1623 mL | |
| 40 mM | 0.0649 mL | 0.3243 mL | 0.6487 mL | 1.6217 mL | |
| 50 mM | 0.0519 mL | 0.2595 mL | 0.5190 mL | 1.2974 mL | |
| 60 mM | 0.0432 mL | 0.2162 mL | 0.4325 mL | 1.0812 mL | |
| 80 mM | 0.0324 mL | 0.1622 mL | 0.3243 mL | 0.8109 mL | |
| 100 mM | 0.0259 mL | 0.1297 mL | 0.2595 mL | 0.6487 mL |
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