2. Metabolic Enzyme/Protease NF-κB
  3. Phosphodiesterase (PDE) Heme Oxygenase (HO) NF-κB
  4. Neuroprotective agent 12

Neuroprotective agent 12 是一种具有口服活性和穿透血脑屏障的神经保护剂。Neuroprotective agent 12 具有强效的神经保护作用，并具有强大的抗氧化和抗炎作用。Neuroprotective agent 12 显著抑制谷氨酸和丙烯醛诱导的细胞死亡，降低 PDE4B 的表达，同时升高 HO-1、p-CREB 和 BDNF 的水平。Neuroprotective agent 12 在创伤性脑损伤 (TBI) 小鼠模型中表现出强效的神经保护作用，具有 TBI 和其他中枢神经系统疾病研究潜力。

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Neuroprotective agent 12 Chemical Structure

Neuroprotective agent 12 Chemical Structure

CAS No. : 2522599-69-3

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Neuroprotective agent 12 相关抗体

Top Publications Citing Use of Products

查看 Phosphodiesterase (PDE) 亚型特异性产品:

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PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

查看 Heme Oxygenase (HO) 亚型特异性产品:

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HO-1 HO-2

查看 NF-κB 亚型特异性产品:

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Neuroprotective agent 12 is an orally active and BBB-penetrable neuroprotective agent. Neuroprotective agent 12 has potent neuroprotective effects with robust anti-oxidation and anti-inflammation. Neuroprotective agent 12 significantly inhibits glutamate- and acrolein-induced cell death, reduces PDE4B expression but increases the HO-1, p-CREB and BDNF levels. Neuroprotective agent 12 exhibits potent neuroprotection in traumatic brain injury (TBI) mice model, promising for TBI and other central nervous system diseases[1].

IC50 & Target

PDE4B

 

HO-1

 

体外研究
(In Vitro)

Neuroprotective agent 12 (Compound 5) (24 小时) 可逆转谷氨酸或丙烯醛诱导的 HT22 细胞死亡[1]。
Neuroprotective agent 12 (3-300 μM，0.5-24 小时) 在 100 μM 以下对 HT22 细胞无毒性，且显著降低谷氨酸或丙烯醛诱导的细胞毒性[1]。
Neuroprotective agent 12 与 PDE4D 活性口袋相互作用，但不影响 PDE4B2 和 PDE4D7 的活性[1]。
Neuroprotective agent 12 (1-10 μM，24 小时) 显著提高 HT22 细胞中 p-CREB、BDNF 和 HO-1 的蛋白水平，并通过直接降低 PDE4B 蛋白来调节 PDE/CREB 通路[1]。
Neuroprotective agent 12 (1-10 μM，1 μg/mL LPS，24 小时) 通过调节 NF-κB 通路抑制 LPS 诱导的神经炎症，并以剂量依赖性方式减少 LPS 刺激的 BV2 细胞中 NO 的释放[1]。
Neuroprotective agent 12 具有良好的肠道吸收和血脑屏障渗透性，抑制 CYP2C19、CYP2C9 和 CYP2D6，但不抑制 CYP1A2 和 Pgp 底物，且毒性低 (LD50：300-5000 mg/kg)[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Neuroprotective agent 12 相关抗体:

Cell Viability Assay[1]

Cell Line: HT22 cells
Concentration: 3, 10, 30, 100, and 300 μM
Incubation Time: 0.5, 24 h
Result: Had great neuroprotective activity on glutamate- and acrolein-induced death on HT22 cells.
Protected 75.8% and 100.5% cell viability by glutamate induced at 3 and 10 μM, respectively.
Protected 72.8% and 96.4% cell viability by acrolein induced at 3 and 10 μM, respectively.
Had no cytotoxicity under 100 μM, and Significantly reduced the glutamate- or acrolein-induced cytotoxicity.

Western Blot Analysis[1]

Cell Line: HT22 cells, BV2 cells
Concentration: 1, 3, 10, 30 μM
Incubation Time: 24 h
Result: Significantly increased the protein levels of p-CREB, BDNF and HO-1.
Decreased the protein level of PDE4B.
Notably decreased the nuclear protein level of NF-Κb in LPS-stimulated BV2 cells at 10 μM.

Immunofluorescence[1]

Cell Line: HT22 cells, BV2 cells
Concentration: 3, 10 μM
Incubation Time: 24 h
Result: Significantly increased p-CREB expression.
Inhibited the nuclear translocation of NF-Κb in LPS-stimulated BV2 cells at 10 μM.
体内研究
(In Vivo)

Neuroprotective agent 12 (Compound 5) (5-10 mg/kg，管饲给药，两次，持续 48 小时) 在 TBI 小鼠模型中具有显著的抗缺血活性和 BBB 神经保护作用[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Kun Ming mice (8 weeks old) were shot twice with rubber bullet at right hemisphere (3 mm lateral and 1 mm posterior to the bregma) to establish TBI mice model.[1].
Dosage: 5, 10 mg/kg
Administration: Gavage administration, twice at 0 and 6 h after awaking for 48 h.
Result: Reduced the bleeding area and repaired the damaged BBB in TBI mice model.
Significantly decreased the hemorrhagic area in a dose-dependent manner in TBI mice model.
Effectively attenuated the Evans Blue leakage induced by TBI.
Reduced the protein levels of MMP2 and MMP9 in TBI mice model.
分子量

380.48

Formula

C23H28N2O3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Neuroprotective agent 12 相关分类

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Keywords:

Neuroprotective agent 122522599-69-3Neuroprotective agent12Neuroprotective agent-12Phosphodiesterase (PDE)Heme Oxygenase (HO)NF-κBHeme OxygenaseNuclear factor-κBNuclear factor-kappaBNeuroprotective agentOxidative stressAnti-inflammationHT22 cellsBV2 cellsTBI mice modelInhibitorinhibitorinhibit

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