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Purity: ≥98%
C-DIM12 is a novel, pphytochemical-based Nurr1 activator with neuroprotective properties. In bladder cancer cells and tumors, it activates the Nurr1-mediated apoptosis axis while suppressing NF-B-dependent gene expression in glial cells. In primary neurons and cell lines, C-DIM12 increases Nurr1 and DA gene expression. In vitro, C-DIM12 increases the expression of dopaminergic genes and guards against 6-hydroxydopamine neurotoxicity. In the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) model of PD in mice, C-DIM12 activates Nurr1 in cancer cells and prevents the loss of dopaminergic neurons. C-DIM12 improved neuronal survival after exposure to 6-OHDA and increased expression of transfected human Nurr1 and Nurr1 protein in primary dopaminergic neurons. These findings suggest that C-DIM12 promotes the expression of Nurr1-regulated genes that are neuroprotective in DA neurons.
Targets |
Nurr1
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ln Vitro |
C-DIM12 induces Nurr1 and DA gene expression in cell lines and primary neurons[3]. In vitro, C-DIM12 inhibits astrocyte inflammatory signaling. Nitric oxide synthase (NOS2), interleukin-6 (IL-6), and chemokine (C-C motif) ligand 2 (CCL2) are NF-B-regulated genes that are inhibited by lipopolysaccharide (LPS) in BV-2 microglia. Nurr1-RNA interference attenuated these effects. Additionally, C-DIM12 increased nuclear translocation of Nurr1 primary microglia while decreasing NF-B activation in NF-B-GFP reporter cells. C-DIM12 increases Nurr1 binding to the p65-binding site while decreasing lipopolysaccharide-induced p65 binding to the NOS2 promoter. Additionally, CoREST (Corepressor for Repressor Element 1 Silencing Transcription Factor) and NCOR2 (Nuclear Receptor Corepressor 2) binding was stabilized by C-DIM12[2].
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ln Vivo |
C-DIM12 has the neuroprotective activity in MPTPp-treated mice[2].
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Cell Assay |
For up to 24 hours, NF-B-GFP HEK cells are exposed to 30 ng/ml of TNF in the presence of 100 μM C-DIM12. C-DIM12 effectively inhibits NF-B-GFP expression in the NF-B-GFP HEK cells after TNF treatment, showing a statistically significant decrease in total GFP fluorescence per cell.
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Animal Protocol |
Transgenic NF-κB/EGFP reporter mice (C57Bl/6 background)
50 mg/kg oral administration IV, Oral gavage |
References |
Molecular Formula |
C23H17CLN2
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Molecular Weight |
356.85
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Exact Mass |
356.108
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Elemental Analysis |
C, 77.41; H, 4.80; Cl, 9.93; N, 7.85
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CAS # |
178946-89-9
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Related CAS # |
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Appearance |
Light Brown solid powder
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SMILES |
CC(=O)O[C@@]12[C@@H]3[C@@H](C[C@@]([C@@H]3OC(=O)C4=CC=CC=C4)([C@H]([C@@H]1O)OC)O)[C@]56[C@H](CC[C@@]7([C@H]5[C@H]([C@H]2C6N(C7)C)OC)COC)OC
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InChi Key |
FIDOCHXHMJHKRW-VHQVDBNASA-N
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InChi Code |
InChI=1S/C33H45NO10/c1-17(35)44-33-21-19(14-31(38,28(42-6)26(33)36)27(21)43-29(37)18-10-8-7-9-11-18)32-20(40-4)12-13-30(16-39-3)15-34(2)25(32)22(33)23(41-5)24(30)32/h7-11,19-28,36,38H,12-16H2,1-6H3/t19-,20+,21-,22+,23+,24-,25?,26+,27-,28+,30+,31-,32+,33-/m1/s1
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Chemical Name |
[(1S,2R,3R,4R,5R,6S,7S,8R,9R,13S,16S,17R,18R)-8-acetyloxy-5,7-dihydroxy-6,16,18-trimethoxy-13-(methoxymethyl)-11-methyl-11-azahexacyclo[7.7.2.12,5.01,10.03,8.013,17]nonadecan-4-yl] benzoate
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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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
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] 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). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.8023 mL | 14.0115 mL | 28.0230 mL | |
5 mM | 0.5605 mL | 2.8023 mL | 5.6046 mL | |
10 mM | 0.2802 mL | 1.4011 mL | 2.8023 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
C-DIM12 induces expression of Nurr1-regulated genes in dopaminergic cell lines by Nurr1 dependent mechanism.Neurosci Lett.2015 Oct 21;607:83-89. doi th> |
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C-DIM12 induces expression of tranfected human Nurr1 in N2A cells and induces expression of TH in primary dopaminergic neurons.Neurosci Lett.2015 Oct 21;607:83-89. doi td> |
Treatment with C-DIM12 is neuroprotective against 6-hydroxydopamine in MN9D and N2A cells.Neurosci Lett.2015 Oct 21;607:83-89. doi td> |