Physicochemical Properties
| Molecular Formula | C32H30FN7O3 |
| Molecular Weight | 579.62 |
| Appearance | Typically exists as solid at room temperature |
| HS Tariff Code | 2934.99.9001 |
| Storage |
Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| Targets | JNK3 21 nM (IC50) JNK2 2203 nM (IC50) JNK1 >10000 nM (IC50) |
| ln Vitro | JNK3 inhibitor-8 (compound 3h; 10, 20 µM; 24, 48 h) enhances the rat cortical neurons' cell survival when they are exposed to 10 µM amyloid-β1-42 [1]. The expression of pc-jun(S63), pc-jun(S73), PARP, and p-Tau is reduced by JNK3 inhibitor-8(10, 20 µM) when treated with 10 µM amyloid-β1-42[1]. |
| ln Vivo | In mice, JNK3 inhibitor-8 (30, 60 mg/kg; oral; once daily for 4 weeks) greatly protects neurons [1]. |
| Cell Assay |
Cell Viability Assay[1] Cell Types: primary rat cortex neuron cells Tested Concentrations: 10, 20 µM Incubation Duration: 24, 48 h Experimental Results: Increased cell viability when treated with 10 µM amyloid-β1-42. Western Blot Analysis[1] Cell Types: primary rat cortex neuron cells Tested Concentrations: 10, 20 µM Incubation Duration: Experimental Results: diminished the expression of pc-jun(S63) and pc-jun(S73) in 0.5 μM anisomycin or 10 μM amyloid-β1-42 stitumed, and diminished the expression of PARP and p-Tau expression when treated with 10 μM amyloid-β1-42. |
| Animal Protocol |
Animal/Disease Models: 6 month-old APP/PS1 AD mice[1] Doses: 30, 60 mg/kg Route of Administration: Po; daily for 4 weeks Experimental Results: Decrease in escape time and distance traveled, demonstrated a Dramatically higher level of altered behavioral ability compared to APP/PS1 and vehicle control in the Y-maze test, improved memory and cognitive function. Animal/Disease Models: 10 month-old 3xTg AD mice[1] Doses: 30, 60 mg/kg Route of Administration: Po; daily for 4 weeks Experimental Results: diminished the escape time and the distance, increased TSPQ and TSTZ levels, Dramatically diminished the expression of pTau levels and improved memory and cognitive function. |
| References |
[1]. Carbamate JNK3 Inhibitors Show Promise as Effective Treatments for Alzheimer's Disease: In Vivo Studies on Mouse Models. J Med Chem. 2023 Apr 24. |
Solubility Data
| Solubility (In Vitro) | May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples |
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples. Injection Formulations (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] *Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7253 mL | 8.6263 mL | 17.2527 mL | |
| 5 mM | 0.3451 mL | 1.7253 mL | 3.4505 mL | |
| 10 mM | 0.1725 mL | 0.8626 mL | 1.7253 mL |