C-DIM12 is Nurr1 activator that stimulates Nurr1 mediated apoptosis axis in bladder cancer cells and tumors and inhibits NF-κB–dependent gene expression in glial cells. C-DIM12 induces Nurr1 and DA gene expression in cell lines and primary neurons. C-DIM12 suppresses astrocyte inflammatory signaling in vitro. C-DIM12 inhibits lipopolysaccharide (LPS)–induced expression of NF-κB-regulated genes in BV-2 microglia including nitric oxide synthase (NOS2), interleukin-6 (IL-6), and chemokine (C-C motif) ligand 2 (CCL2), and the effects were attenuated by Nurr1-RNA interference. C-DIM12 has the neuroprotective activity in MPTPp-treated mice.
| Cell Experiment | |
|---|---|
| Cell lines | HEK293 cells |
| Preparation method | C-DIM12 is efficient at blocking NF-κB–GFP expression in the NF-κB–GFP HEK cells after TNFα treatment, displaying a statistically significant reduction in total GFP fluorescence per cell. NF-κB–GFP HEK cells are exposed to 30 ng/ml of TNFα in the presence of 100 μM C-DIM12 for up to 24 hours. |
| Concentrations | 100 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | Transgenic NF-κB/EGFP reporter mice |
| Formulation | corn oil |
| Dosages | 50 mg/kg |
| Administration | oral |
| Molecular Weight | 356.85 |
| Formula | C23H17ClN2 |
| CAS Number | 178946-89-9 |
| Form | Solid |
| Solubility (25°C) | DMSO 70 mg/mL Ethanol 70 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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