C-DIM12
Based on 2 publication(s) in Google Scholar
C-DIM12 is a potent, orally active Nurr1 modulator. C-DIM12 inhibits the tumor growth and autophagy, and induces the cell apoptosis. C-DIM12 has anti-inflammatory and neuroprotective effects, and can be used for cancer and neurological disease study.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.01%
- CAS 番号: 178946-89-9
- 分子式: C23H17ClN2
- 分子量:356.85
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
MedChemExpress(MCE)の使用を引用している文献 C-DIM12
MoreNuclear Hormone Receptor 4A/NR4A アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
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Nurr1/NR4A2 |
体外実験
体内実験
C-DIM12 (50-100 mg/kg for i.p., three times ) attenuates brain inflammation and improves functional recovery after intracerebral hemorrhage in mice[3].
C-DIM12 (30 mg/kg for i.p., 30 day) inhibits tumor growth and autophagy, and induces apoptosis in NURR1-KO cells orthotopic xenograft[1].
Pharmacokinetic Analysis in C57BL/6 male mice[1]
| Route | Organ | Dose (mg/kg) | Area under Curve (ng/mL*min) | t1/2 (min) | Cmax (ng/mL) |
| i.g. | Plasma | 25 | 539,220 | 249 | 1120 |
| i.g. | Brain | 25 | 2,273,711 | 265 | 3622 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MPTP-induced C57BL/6 male Parkinsonism mice [2]
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Dosage:25 mg/kg/day, 14day
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Administration:Intragastric gavage (i.g.)
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Result:Protected against the loss of DA neurons in the substantia nigra pars compacta and DA terminals in the striatum, maintained a ramified phenotype in microglia, and suppressed activation of astrocytes.
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Animal Model:The ICR mice model of intracerebral hemorrhage induced by collagenase type VII[3]
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Dosage:50 and 100mg/kg/day at a 24-h interval, three times
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Administration:Orally administration
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Result:Improved the recovery of neurological function and prevented neuron loss in the hematoma, while suppressed activation of microglia/macrophages and expression of inflammatory mediators interleukin-6 and CC chemokine ligand 2.
Preserved axonal structures in the internal capsule and axonal transport function.
Decreased of iNOS mRNA expression.
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Animal Model:MiaPaCa2 cells (Ctrl and NURR1-KO) orthotopic xenograft tumor models[1]
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Dosage:30 mg/kg, 30 day
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Administration:Intraperitoneal injection (i.p.)
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Result:Inhibited tumor growth and ATG7 and ATG12 mRNA levels, and induced apoptosis.
化学情報
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CAS 番号 178946-89-9
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性状 Solid
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分子量 356.85
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分子式 C23H17ClN2
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Color Light yellow to brown
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SMILES
ClC1=CC=C(C(C2=CNC3=C2C=CC=C3)C4=CNC5=C4C=CC=C5)C=C1
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別名
DIM-C-pPhCl
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (2)
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Journal Impact Factor
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Most Recent
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J Immunol
NR4A nuclear receptor expression in human macrophages mediates apoptosis and controls Mycobacterium tuberculosis growth. [Abstract]2025 Sep 26:vkaf252. PMID: 41005755 -
溶剤 & 溶解度
体外:
DMSO : ≥ 100 mg/mL (280.23 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (7.01 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (289 KB)
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SDS (393 KB)
- English - EN (393 KB)
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- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Zarei M, et al. Nuclear Receptor 4A2 (NR4A2/NURR1) Regulates Autophagy and Chemoresistance in Pancreatic Ductal Adenocarcinoma. Cancer Res Commun. 2021;1(2):65-78. [Content Brief]
[4]. De Miranda BR, et al. The Nurr1 Activator 1,1-Bis(3'-Indolyl)-1-(p-Chlorophenyl)Methane Blocks Inflammatory Gene Expression in BV-2 Microglial Cells by Inhibiting Nuclear Factor κB. Mol Pharmacol. 2015 Jun;87(6):1021-34. doi: 10.1124/mol.114.095398. Epub 2015 Apr 9. [Content Brief]
[5]. Hammond SL, et al. A novel synthetic activator of Nurr1 induces dopaminergic gene expression and protects against 6-hydroxydopamine neurotoxicity in vitro. Neurosci Lett. 2015 Oct 21;607:83-9. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8023 mL | 14.0115 mL | 28.0230 mL | 70.0574 mL |
| 5 mM | 0.5605 mL | 2.8023 mL | 5.6046 mL | 14.0115 mL | |
| 10 mM | 0.2802 mL | 1.4011 mL | 2.8023 mL | 7.0057 mL | |
| 15 mM | 0.1868 mL | 0.9341 mL | 1.8682 mL | 4.6705 mL | |
| 20 mM | 0.1401 mL | 0.7006 mL | 1.4011 mL | 3.5029 mL | |
| 25 mM | 0.1121 mL | 0.5605 mL | 1.1209 mL | 2.8023 mL | |
| 30 mM | 0.0934 mL | 0.4670 mL | 0.9341 mL | 2.3352 mL | |
| 40 mM | 0.0701 mL | 0.3503 mL | 0.7006 mL | 1.7514 mL | |
| 50 mM | 0.0560 mL | 0.2802 mL | 0.5605 mL | 1.4011 mL | |
| 60 mM | 0.0467 mL | 0.2335 mL | 0.4670 mL | 1.1676 mL | |
| 80 mM | 0.0350 mL | 0.1751 mL | 0.3503 mL | 0.8757 mL | |
| 100 mM | 0.0280 mL | 0.1401 mL | 0.2802 mL | 0.7006 mL |