Nurr1/RXR agonist 1
Based on 1 Customer Validation
Nurr1/RXR dual agonist 1 is a dual activator of Nurr1 (EC50 = 2.6 µM) and RXR with Ks of 0.6 and 1.1 µM, respectively. Nurr1/RXR dual agonist 1 exclusively activates the heterodimer response element DR5 by selectively destabilizing the Nurr1 homodimer and stabilizing the Nurr1:RXR heterodimer. Nurr1/RXR dual agonist 1 enhances expression of a specific subset of neuroprotective Nurr1 target genes while avoiding induction of genes associated with potential off-target effects in neuronal cells. Nurr1/RXR dual agonist 1 can be used for neurodegenerative diseases research.
For research use only. We do not sell to patients.
- Purity: 98.26%
- CAS No.: 2231746-53-3
- Formula: C18H19F2NO2
- Molecular Weight:319.35
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
All Nuclear Hormone Receptor 4A/NR4A Isoforms
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Biological Activity
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Nurr1/NR4A2 |
Nurr1/RXR agonist 1 (compound 2) (15 h) induces a considerable 3.3-fold activation of Nurr1, with both Nurr1 and RXR involved[1].
Nurr1/RXR dual agonist 1 (30 μM) diminishes Nurr1 homodimer formation while leaving the Nurr1:RXR heterodimer intact[1].
Nurr1/RXR agonist 1 (0.3-30 μM) enhances DR5-dependent transcription but does not activate NBRE or NurRE[1].
Nurr1/RXR agonist 1 (0.3-30 μM, 24 h) exhibits no toxic effect in HEK293T cells[1].
Nurr1/RXR agonist 1 (10 μM, 21 h) achieves differential modulation or functional selectivity in activating downstream gene expression programs in rat dopaminergic neurons[1].
Nurr1/RXR agonist 1 induces genes that have a higher empirical probability of containing DR5 elements in their promoter regions[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:rat dopaminergic neurons
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Concentration:10 μM
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Incubation Time:21 h
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Result:Induced the expression of tyrosine hydroxylase (TH), fibronectin leucine rich transmembrane protein 2 (FLRT2), brain-derived neurotrophic factor (BDNF) and collapsin response mediator protein 4 (CRMP4; Dpysl3 in rat).
Did not induced X-linked inhibitor of apoptosis protein (XIAP), sestrin 3 (SESN3), cyclin D2 (CCND2), baculoviral inhibitor of apoptosis repeat-containing 5 (BIRC5), and superoxide dismutase 2 (SOD2).
Chemical Information
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CAS No. 2231746-53-3
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Appearance Solid
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Molecular Weight 319.35
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Formula C18H19F2NO2
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Color White to off-white
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SMILES
O=C(O)CC1=CC=C(N2C(C)=C(C)C3=C2CCC(F)(F)C3)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL (313.14 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). 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). 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 (7.83 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 (7.83 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)
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.
Purity & Documentation
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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). 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 | 3.1314 mL | 15.6568 mL | 31.3136 mL | 78.2840 mL |
| 5 mM | 0.6263 mL | 3.1314 mL | 6.2627 mL | 15.6568 mL | |
| 10 mM | 0.3131 mL | 1.5657 mL | 3.1314 mL | 7.8284 mL | |
| 15 mM | 0.2088 mL | 1.0438 mL | 2.0876 mL | 5.2189 mL | |
| 20 mM | 0.1566 mL | 0.7828 mL | 1.5657 mL | 3.9142 mL | |
| 25 mM | 0.1253 mL | 0.6263 mL | 1.2525 mL | 3.1314 mL | |
| 30 mM | 0.1044 mL | 0.5219 mL | 1.0438 mL | 2.6095 mL | |
| 40 mM | 0.0783 mL | 0.3914 mL | 0.7828 mL | 1.9571 mL | |
| 50 mM | 0.0626 mL | 0.3131 mL | 0.6263 mL | 1.5657 mL | |
| 60 mM | 0.0522 mL | 0.2609 mL | 0.5219 mL | 1.3047 mL | |
| 80 mM | 0.0391 mL | 0.1957 mL | 0.3914 mL | 0.9786 mL | |
| 100 mM | 0.0313 mL | 0.1566 mL | 0.3131 mL | 0.7828 mL |
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