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编 号:F215405
分子式:C23H17ClN2
分子量:356.85
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10mM*1mL in DMSO
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
C-DIM12 is a potent, orally active Nurr1 antagonist. 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.

体内研究:
C-DIM12 (每次 25 mg/kg, 14 天) 改善帕金森小鼠的神经胶质反应性。C-DIM12 (50-100 mg/kg, 每次 3次)可减轻小鼠脑出血后脑炎症,促进功能恢复。C-DIM12 (30 mg/kg, 腹腔注射,30 天) 抑制 NURR1-KO 细胞原位异种移植裸鼠的肿瘤生长和自噬现象,促进细胞凋亡。在C57BL/6雄性小鼠中的药代动力学分析RouteOrganDose (mg/kg)Area under Curve (ng/mL*min)t1/2 (min)Cmax (ng/mL)
i.g.Plasma25539,2202491120
i.g.Brain252,273,7112653622
Animal Model:MPTP-induced C57BL/6 male Parkinsonism mice
Dosage:25 mg/kg/day, 14day
Administration:Intragastric gavage (i.g.)
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.
Animal Model:The ICR mice model of intracerebral hemorrhage induced by collagenase type VII
Dosage:50 and 100mg/kg/day at a 24-h interval, three times
Administration:Orally administration
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.
Animal Model:MiaPaCa2 cells (Ctrl and NURR1-KO) orthotopic xenograft tumor models
Dosage:30 mg/kg, 30 day
Administration:Intraperitoneal injection (i.p.)
Result:Inhibited tumor growth and ATG7 and ATG12 mRNA levels, and induced apoptosis.

体外研究:
C-DIM12 (15 μM, 3-5 天) 通过抑制细胞自噬降低 MiaPaCa2 细胞的增殖和存活。
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