DN-1289 |
Catalog No.GC71195
One-Click Copy Product Info
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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).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 3026597-15-6
Sample solution is provided at 25 µL, 10mM.
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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.
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].
DN-1289 (compound 14) (100 mg/kg and 150 mg/kg; i.p.; once daily for 10-15 d) is well-tolerated in mice model[1].
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 | / | / | / |
GLPBIO has not independently confirmed the accuracy of these methods. They are for reference only.
References:
[1]. Craig RA 2nd, et al. Discovery of Potent and Selective Dual Leucine Zipper Kinase/Leucine Zipper-Bearing Kinase Inhibitors with Neuroprotective Properties in In Vitro and In Vivo Models of Amyotrophic Lateral Sclerosis. J Med Chem. 2022 Dec 22;65(24):16290-16312.
| Cas No. | 3026597-15-6 | SDF | |
| Formula | C18H19F4N7O2 | M.Wt | 441.38 |
| Solubility | Storage | ||
| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2656 mL | 11.3281 mL | 22.6562 mL |
| 5 mM | 453.1 μL | 2.2656 mL | 4.5312 mL |
| 10 mM | 226.6 μL | 1.1328 mL | 2.2656 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 saline, 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:
- Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)