Physicochemical Properties
| CAS # | 2873465-25-7 |
| 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 4.1 nM (IC50) JNK2 44 nM (IC50) JNK1 147.8 nM (IC50) |
| ln Vitro | The IC50 values of JNK3 inhibitor-3 (0-10 μM) are 4.1 nM, 44.0 nM, and 147.8, respectively, indicating that it has inhibitory actions against JNK1, JNK2, and JNK3. In vitro, JNK3 inhibitor-3 (20 μM; 24 and 48 hours) exhibits neuroprotective properties[1]. |
| ln Vivo | The memory of the 3xTg mice dementia model is improved by JNK3 inhibitor-3 (30 and 60 mg/kg; oral dosing, once day for 2 or 2.2 month)[1]. 1.19 JNK3 inhibitor-3's Pharmacokinetic Properties in Rats[1]. AUC (hr·ng/mL) 1085.24 2806.77 Cmax (ng/mL) 1238.85 Tmax (hr) 0.67 T1/2 (hr) 0.36 1.14 BA (%) 86.21 Rats IV 1 mg/kg Rats PO 3 mg/kg |
| Cell Assay |
Cell Viability Assay[1] Cell Types: Rat cortical neurons Tested Concentrations: 20 μM Incubation Duration: 24 and 48 hrs (hours) Experimental Results: Protected rat cortical neurons against 10 μM Aβ1-42 induced neurotoxicity. |
| Animal Protocol |
Animal/Disease Models: Homozygous 3xTg and APPswe/PS1dE9 double-transgenic mice model of Alzheimer's disease[1] Doses: 30 and 60 mg/kg Route of Administration: Oral administration; one time/day for 2 or 2.2 month Experimental Results: Induced no abnormal symptoms or weight changes, Dramatically enhanced the spontaneous alteration in APP/PS1 and doses of 30 and 60 mg/kg than that of vehicle group in Y-maze test and demonstrated a significant difference compared to the 3xTg vehicle control in the passive avoidance test. |
| References |
[1]. Discovery of novel imidazole chemotypes as isoform-selective JNK3 inhibitors for the treatment of Alzheimer's disease. Eur J Med Chem. 2023 Jan 5;245(Pt 1):114894. |
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.) |