DN-1289
Based on 1 publication(s) in Google Scholar
DN-1289 is an orally active and selective inhibitor of dual leucine zipper kinase (DLK; IC50=17 nM) and leucine zipper-bearing kinase (LZK; IC50=40 nM). DN-1289 results significant attenuation of optic nerve crush (ONC)-induced p-c-Jun in mice model. DN-1289 has excellent in vivo plasma half-life and blood-brain barrier permeability.
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- Pureza: 99.63%
- No. CAS: 3026597-15-6
- Fòrmula: C18H19F4N7O2
- Peso molecular:441.38
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) DN-1289
More
Actividad biológica
IC50: 17 nM (DLK), 40 nM (LZK)[1]
DN-1289 (compound 14) (0.1, 0.3, and 1 μM; 0-20 h) can block axon degeneration in dorsal root ganglion (DRG) neurons induced by nerve growth factor (NGF) withdrawal[1].
DN-1289 (0.1, 0.3, and 1 μM; 0-20 h) inhibits the activation of caspases in DRG neurons over time induced by NGF withdrawal[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
DN-1289 (150 mg/kg; p.o.; b.i.d. for 10 d) inhibits phosphorylation of c-Jun in an acute injury model with optic nerve crush (ONC) application[1].
Pharmacokinetic Analysis[1]
| Species | Route | Dose (mg/kg) | plasma Cmax (μM) | plasma AUC0-24 h (μM·h) | CLp (mL/min/kg) | CLu (mL/min/kg) | Vd (L/kg) | t1/2 (h) | F (%) | Kpuu (AUC) | brain AUC0-2 h (μM·h) |
| rat | IV | 1 | 1.09 | 2.42 | 14.7 | 150 | 6.7 | 6.5 | / | 0.6 | 4.05 |
| PO | 3 | 0.58 | 3.9 | / | / | / | 4.6 | 52 | / | / | |
| mouse | IV | 1 | 1.06 | 4.06 | 8.6 | 200 | 4.7 | 6.8 | / | / | / |
| PO | 10 | 2.32 | 21.9 | / | / | / | 7.9 | 56 | 0.4 | 6.91 | |
| PO | 150 | 24.9 | 324 | / | / | / | 23.7 | 53 | / | / | |
| IP | 100 | 15.4 | 280 | / | / | / | 23.7 | 53 | / | / | |
| cyno | IV | 0.5 | 0.746 | 2.79 | 6.1 | 64 | 3.4 | 7.9 | / | / | / |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 3026597-15-6
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Appearance Solid
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Peso molecular 441.38
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Fòrmula C18H19F4N7O2
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Color White to off-white
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SMILES
NC1=C(OC(F)F)N=C(C2=NC(N3[C@@H](C4)CO[C@@H]4C3)=NC(N5CCC(F)(F)C5)=C2)C=N1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
Solvente y solubilidad
DMSO : 100 mg/mL (226.56 mM; ultrasonic and warming and heat to 60°C; 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. 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. 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 (5.66 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 (5.66 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.
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.
Pureza y Documentación
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Ficha de datos (281 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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. 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 | 2.2656 mL | 11.3281 mL | 22.6562 mL | 56.6405 mL |
| 5 mM | 0.4531 mL | 2.2656 mL | 4.5312 mL | 11.3281 mL | |
| 10 mM | 0.2266 mL | 1.1328 mL | 2.2656 mL | 5.6641 mL | |
| 15 mM | 0.1510 mL | 0.7552 mL | 1.5104 mL | 3.7760 mL | |
| 20 mM | 0.1133 mL | 0.5664 mL | 1.1328 mL | 2.8320 mL | |
| 25 mM | 0.0906 mL | 0.4531 mL | 0.9062 mL | 2.2656 mL | |
| 30 mM | 0.0755 mL | 0.3776 mL | 0.7552 mL | 1.8880 mL | |
| 40 mM | 0.0566 mL | 0.2832 mL | 0.5664 mL | 1.4160 mL | |
| 50 mM | 0.0453 mL | 0.2266 mL | 0.4531 mL | 1.1328 mL | |
| 60 mM | 0.0378 mL | 0.1888 mL | 0.3776 mL | 0.9440 mL | |
| 80 mM | 0.0283 mL | 0.1416 mL | 0.2832 mL | 0.7080 mL | |
| 100 mM | 0.0227 mL | 0.1133 mL | 0.2266 mL | 0.5664 mL |
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