2. Apoptosis Neuronal Signaling GPCR/G Protein Immunology/Inflammation
  3. Apoptosis Cholinesterase (ChE) Tau Protein Ferroptosis Histamine Receptor
  4. H3R antagonist 4

H3R antagonist 4 (compound 11l) 是胆碱酯酶和组胺 H3 受体 (H3R) 的双重抑制剂，对应的 IC50 分别为 7.04 μM (eeAChE)，9.73 μM (hAChE)(可逆)，1.09 nM (H3R)。H3R antagonist 4 对自身和 Cu2+ 诱导的 Aβ1-42 聚集有良好的抑制作用 (95.48% 和 88.63%)，和对自身和 Cu2+ 诱导的 Aβ1-42 原纤维具有良好的降解作用 (80.16%和89.30%)。H3R antagonist 4 有螯合 Cu2+、Zn2+、Al3+ 和 Fe2+ 等生物金属的能力。H3R antagonist 4 显著降低了 Aβ1-42 诱导的 tau 蛋白过度磷酸化，抑制 RSL-3 诱导的 PC12 细胞凋亡和铁死亡。H3R antagonist 4 在 hCMEC/D3 和 hPepT1-MDCK 细胞中有最佳的血脑屏障通透性和肠道吸收特性。H3R antagonist 4 可改善利用东莨菪碱 (HY-N0296) 诱导的阿尔兹海默症小鼠模型的学习和记忆障碍。

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H3R antagonist 4 Chemical Structure

H3R antagonist 4 Chemical Structure

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H3R antagonist 4 相关抗体

Top Publications Citing Use of Products

查看 Cholinesterase (ChE) 亚型特异性产品:

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

H3R antagonist 4 (compound 11L) was a dual inhibitor of cholinesterase and histamine receptor (H3R), with corresponding IC50 of 7.04 μM (eeAChE), 9.73 μM (hAChE)(reversible) and 1.09 nM (H3R) , respectively. H3R antagonist 4 inhibited the aggregation of Aβ1-42 induced by itself and Cu2+ (95.48% and 88.63%) , and degraded the Aβ1-42 fibrils induced by itself and Cu2+ (80.16% and 89.30%) . H3R antagonist 4 chelate biometals such as Cu2+, Zn2+, Al3+, and Fe2+. H3R antagonist 4 significantly reduced tau protein hyperphosphorylation induced by Aβ1-42 and inhibited RSL-3-induced apoptosis and ferroptosis in PC12 cells. H3R antagonist 4 had the best blood-brain barrier permeability and intestinal absorption in hCMEC/D3 and hPepT1-MDCK cells.H3R antagonist 4 ameliorates learning and memory impairment in a mouse model of Alzheimer's disease induced by scopolamine (HY-N0296) [1] .

IC50 & Target

hAChE

9.73 μM (IC50)

EeAChE

7.04 μM (IC50)

eqBCHE

13.40 ~ 88 μM (IC50)

体外研究
(In Vitro)

H3R antagonist 4（compound 11l）对eeAChE，eqBuChE 和 hAChE 有抑制作用，对应的 IC50 分别为 7.04 μM，13.40 μM 和 9.73 μM 且对 huAChE 抑制机制是可逆的[1] 。
H3R antagonist 4 与 AChE 结合，占据酶促CAS、midgorge位点和PAS。与 huAChE 的阴离子活性中心和外周阴离子位点相互作用，可同时结合 CAS和 PAS 位点作为双位点 AChE 抑制剂[1] 。
H3R antagonist 4 对自身和 Cu2+ 诱导的 Aβ1-42 聚集有良好的抑制作用 (95.48%和88.63%) (ThT fluorescence assay)，和对自身和 Cu2+ 诱导的 Aβ1-42 原纤维具有良好的降解作用 (80.16%和89.30%)(TEM)[1]。
H3R antagonist 4 (TRFRET) 抑制 H3R 的 IC50 为 1.09 nM[1]。
H3R antagonist 4 (5 µM，10 µM 和 20 µM) (WB) 在 PC12 细胞中可抑制异常的 tau 磷酸化[1]。
H3R antagonist 4 (11 μM) 提高 PC12 (经 800 μM H2O2) 存活率为 75.66%，降低了 ROS 水平。通过降低 ROS 积累来保护 PC12 细胞免受 H2O2影响，凋亡细胞比例显著增加，达到 22.9%±0.36%[1]。
H3R antagonist 4 (5，10，20 μM) 抑制 RSL3 诱导的 PC12 细胞铁死亡，显著提高了细胞活力。诱导的损伤提高体外血脑屏障通透性[1]。
H3R antagonist 4（UV–vis spectrometry）可螯合 Cu2+、Zn2+、Al3+ 和 Fe2+ 等生物金属[1]。
H3R antagonist 4 在 hPepT1-MDCK 细胞中提高 PepT1 的蛋白表达[1]。
H3R antagonist 4 (0 - 80 μM，1h) 在 BV-2 细胞中显示抗炎作用且不影响增殖[1]。

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

H3R antagonist 4 相关抗体:

Western Blot Analysis[1]

Cell Line: PC12
Concentration: 5, 10, 20 μM; Aβ25-35
Incubation Time: 30 min
Result: Inhibited tau hyperphosphorylation, the relative protein expression of p-Tau (Thr 181)/Total-tau significantly increased.

Apoptosis Analysis[1]

Cell Line: PC12
Concentration: 5, 10, 20 μM; H2O2, 800 μM, 4 h
Incubation Time: 24 h
Result: Reduced the apoptosis of PC12 cells.

Cell Viability Assay[1]

Cell Line: BV-2
Concentration: 0 - 80 μM; LPS 10 μg/mL; treated with all result.
Incubation Time: 1 h
Result: Reduced inflammation.

Cell Viability Assay[1]

Cell Line: PC12
Concentration: 5, 10, 20 µM; H2O2, 800 μM, 4 h
Incubation Time: 24 h
Result: Increased cell viability to 75.66 %.
体内研究
(In Vivo)

H3R antagonist 4 (compound 11l) (2.5和5.0 mg/kg) 能有效改善东莨菪碱（HY-N0296）诱导的神经细胞病理形态学改变，可显著改善AD模型小鼠的认知缺陷和空间记忆[1]。
H3R antagonist 4(compound 11l) pharmacokinetics form[1]

H3R antagonist 4 (compound 11l)给药后的药代动力学表格[1]

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

Parameter AUC0→24 MRT0→24 t1/2 Vd
102.24 ± 19.07μg/mL•min 39.17 ± 2.50min 138.64 ± 17.69min 9.21 ± 0.43L/kg
Animal Model: AD mouse model[1]
Dosage: 2.5 and 5.0 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Reduced AChE activity and ACh levels increased in the rivastigmine.Hematoxylin and eosin (HE) staining showed that hippocampal cells in the model group were loosely arranged and disorganized, and that the number of cells was reduced.Significantly improved cognitive deficits and spatial memory in AD model mice. A good pharmacokinetic profile of H3R antagonist 4 was confirmed in an in vivo study [1].
Animal Model: SD mouse model (200-220 g)[1]
Dosage: Fasted for 12 h; 10 and 17 mg/kg
Administration: Intravenous injection (i.v.)
Result: Good blood-brain barrier permeability.
Animal Model: SD mouse model[1]
Dosage: 1.25, 2.5, 5.0 mg/kg; scopolamine, 1.25 mg/kg, Intraperitoneal injection
Administration: i.g.
Result: Shortened the escape latency compared with the model group. Improved the learning and memory ability of scopolamine-injected mice [1].
分子量

568.61

Formula

C30H36N2O9
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

H3R antagonist 4 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

H3R antagonist 4ApoptosisCholinesterase (ChE)Tau ProteinFerroptosisHistamine ReceptorAntioxidant activityH3R receptor antagonistic activityNeuroprotective effects of cell damagePC12 cellsReactive oxygen species productionBlood-brain barrier permeability in vitroAnti-inflammatory in vitroInhibitorinhibitorinhibit

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