DIM-C-pPhOCH3
(Synonyms: DIM-C-pPhOCH3) 目录号 : GC32884
A Nur77 receptor agonist
Cas No.:33985-68-1
Sample solution is provided at 25 µL, 10mM.
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C-DIM5 is a para-phenyl-substituted diindolylmethane (C-DIM) and an agonist of the orphan receptor nuclear receptor-related protein 77 (Nur77).1 It selectively activates Nur77 over peroxisome proliferator receptor γ (PPARγ) in reporter assays when used at a concentration of 20 μM. C-DIM5 (10, 15, and 20 μM) inhibits growth of and induces apoptosis in L3.6pL pancreatic cancer cells.2 It stabilizes nuclear localization of Nur77 and Nurr1 and reduces secretion of the pro-inflammatory cytokines IL-2, IL-6, IL-12p70, CCL2, and CCL5 in primary mouse astrocytes.3 Oral administration of C-DIM5 (50 mg/kg) prevents loss of dopaminergic neurons in the substantia nigra pars compacta and striatal dopamine terminals in a mouse model of Parkinson's disease induced by MPTP.4
1.Chintharlapalli, S., Burghardt, R., Papineni, S., et al.Activation of Nur77 by selected 1,1-Bis(3'-indolyl)-1-(p-substituted phenyl)methanes induces apoptosis through nuclear pathwaysJ. Biol. Chem.280(26)24903-24914(2005) 2.Yoon, K., Lee, S.O., Cho, S.D., et al.Activation of nuclear TR3 (NR4A1) by a diindolylmethane analog induces apoptosis and proapoptotic genes in pancreatic cancer cells and tumorsCarcinogenesis32(6)836-842(2011) 3.Popichak, K.A., Hammond, S.L., Moreno, J.A., et al.Compensatory expression of Nur77 and Nurr1 regulates NF-κB-dependent inflammatory signaling in astrocytesMol. Pharmacol.94(4)1174-1186(2018) 4.De Miranda, B.R., Miller, J.A., Hansen, R.J., et al.Neuroprotective efficacy and pharmacokinetic behavior of novel anti-inflammatory para-phenyl substituted diindolylmethanes in a mouse model of Parkinson's diseaseJ. Pharmacol. Exp. Ther.345(1)125-138(2013)
Cell experiment: | RKO cells are treated with DMSO or 12.5 μM DIM-C-pPhOCH3 for 2 and 6 h. RNA is isolated for the reverse transcription-PCR (RT-PCR) experiment and analyzed for gene expression, and three replicates are determined for each time point and the DMSO control. The microarray data are analyzed[1]. |
Animal experiment: | Mice[1]Male athymic nude mice (Foxn1nu, ages 7-8 weeks) are used. The mice are housed and maintained in laminar flow cabinets under specific pathogen-free conditions. A xenograft is established by s.c. injection of in vitro cultured RKO cells (5×106 per 150 μL) into the flanks of individual mice. Tumors are allowed to grow for 4 days until tumors are palpable. Mice are then randomized into two groups of six mice per group and dosed by oral gavage with either corn oil or 25 mg/kg/d DIM-C-pPhOCH3 for 21 days. The mice are weighed, and tumor size is measured[1]. |
References: [1]. Cho SD, et al. Nur77 agonists induce proapoptotic genes and responses in colon cancer cells through nuclear receptor-dependent and nuclear receptor-independent pathways. Cancer Res. 2007 Jan 15;67(2):674-83. | |
| Cas No. | 33985-68-1 | SDF | |
| 别名 | DIM-C-pPhOCH3 | ||
| Canonical SMILES | COC1=CC=C(C(C2=CNC3=C2C=CC=C3)C4=CNC5=C4C=CC=C5)C=C1 | ||
| 分子式 | C24H20N2O | 分子量 | 352.43 |
| 溶解度 | DMSO : ≥ 33.3 mg/mL (94.49 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8374 mL | 14.1872 mL | 28.3744 mL |
| 5 mM | 0.5675 mL | 2.8374 mL | 5.6749 mL |
| 10 mM | 0.2837 mL | 1.4187 mL | 2.8374 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet