δ-Secretaseinhibitor11

• 常用名: δ-Secretaseinhibitor11
• 英文名: δ-secretase inhibitor 11
• CAS号: 842964-18-5
• 分子量: 220.22800
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₀H₁₂N₄O₂
• 熔点: N/A
• 闪点: N/A

δ-Secretaseinhibitor11用途

δ-分泌酶抑制剂11(化合物11)是一种口服活性、强效、BBB渗透、无毒、选择性和特异性δ-分泌蛋白酶抑制剂,IC50为0.7μM。δ分泌酶抑制剂11与δ分泌酶的活性位点和变构位点相互作用。δ-分泌酶抑制剂11减弱tau和APP(淀粉样前体蛋白)的切割。δ-分泌酶抑制剂11改善tau P301S和5XFAD转基因小鼠模型中的突触功能障碍和认知损伤。δ-分泌酶抑制剂11可用于阿尔茨海默病研究[1]。

δ-Secretaseinhibitor11名称

• 中文名: 7-吗啉-4-基苯并[1,2,5]恶二唑-4-基胺
• 英文名: 7-Morpholin-4-yl-benzo[1,2,5]oxadiazol-4-ylamine

δ-Secretaseinhibitor11生物活性

• 描述: δ-分泌酶抑制剂11(化合物11)是一种口服活性、强效、BBB渗透、无毒、选择性和特异性δ-分泌蛋白酶抑制剂,IC50为0.7μM。δ分泌酶抑制剂11与δ分泌酶的活性位点和变构位点相互作用。δ-分泌酶抑制剂11减弱tau和APP(淀粉样前体蛋白)的切割。δ-分泌酶抑制剂11改善tau P301S和5XFAD转基因小鼠模型中的突触功能障碍和认知损伤。δ-分泌酶抑制剂11可用于阿尔茨海默病研究[1]。
• 相关类别:
  信号通路 >> 细胞凋亡 >> 胱天蛋白酶
  研究领域 >> 神经疾病
• 靶点实验:

  Caspase-3:31.86 ± 1. μM (IC50)

  Caspase-8:86.71 ± 10 μM (IC50)

• 体外研究: δ-分泌酶抑制剂11(化合物11)(0-1μM,10min)以浓度和时间依赖性方式抑制δ-分泌蛋白酶[1]。δ-分泌酶抑制剂11(0-1μ。
• 体内研究: δ-分泌酶抑制剂11(化合物11)(10mg/kg,口服,每日一次,持续3个月)可减轻OGD(氧-葡萄糖剥夺)诱导的神经元损伤,并特别发挥神经保护作用[1]。δ-分泌酶抑制剂11(0-10 mg/kg,口服,每日1次,持续1.5和3个月)抑制δ-分泌活性,减轻5XFAD小鼠模型中的Aβ沉积和认知缺陷[1]。动物模型：Tau P301S转基因小鼠(每组4只小鼠)[1]剂量：10mg/kg给药：口服,每日1次,连续3个月结果：显著抑制野生型和Tau P301 S小鼠脑中δ-分泌酶的活性,增加PP2A活性,并减弱Tau P30S小鼠中Tau的截短和磷酸化。改善tau P301S小鼠的突触丢失并恢复突触功能障碍。动物模型：5XFAD小鼠[1]剂量：2、5或10 镁 kg给药：口服,每日1次,持续1.5和3个月。结果：减弱β-分泌酶介导的APP处理,显著降低脑溶解物中Aβ1-40和Aβ1-42的浓度,并以时间和剂量依赖性方式减弱Aβ沉积。
• 参考文献:

  [1]. Zhang Z, et al. Inhibition of delta-secretase improves cognitive functions in mouse models of Alzheimer's disease. Nat Commun. 2017 Mar 27;8:14740.

δ-Secretaseinhibitor11物理化学性质

• 分子式: C₁₀H₁₂N₄O₂
• 分子量: 220.22800
• 精确质量: 220.09600
• PSA: 77.41000
• LogP: 1.28780
• InChIKey: LWCSTSZSZFUHAT-UHFFFAOYSA-N
• SMILES: Nc1ccc(N2CCOCC2)c2nonc12
• 储存条件: 室温

δ-Secretaseinhibitor11安全信息

• 海关编码: 2934999090

δ-Secretaseinhibitor11海关

• 海关编码: 2934999090
• 中文概述: 2934999090. 其他杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%
• 申报要素: 品名, 成分含量, 用途
• Summary: 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

δ-Secretaseinhibitor11靶点实验

查看更多实验

实验名称：Primary cell-based high-throughput screening assay for identification of compounds th... 来源：Johns Hopkins Ion Channel Center 靶标：regulator of G-protein signaling 4 isoform 2 [Homo sapiens] External Id：JHICC_RGS_Act_HTS

实验名称：Luminescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：mu-type opioid receptor isoform MOR-1 [Homo sapiens] External Id：OPRM1-OPRD1_AG_LUMI_1536_1X%ACT PRUN

实验名称：QFRET-based biochemical primary high throughput screening assay to identify exosite i... 来源：The Scripps Research Institute Molecular Screening Center 靶标：disintegrin and metalloproteinase domain-containing protein 17 preproprotein [Homo sapiens] External Id：ADAM17_INH_QFRET_1536_1X%INH PRUN

实验名称：Fluorescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：muscarinic acetylcholine receptor M1 [Homo sapiens] External Id：CHRM1_AG_FLUO8_1536_1X%ACT PRUN

实验名称：uHTS identification of small molecule activators of the adaptive arm of the Unfolded ... 来源：Burnham Center for Chemical Genomics 靶标：N/A External Id：BCCG-A405-UPR-XBP1-PrimaryAgonist-Assay

实验名称：A screen for compounds that inhibit the activity of LtaS in Staphylococcus aureus 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School External Id：HMS979

实验名称：High throughput fluorescence intensity-based biochemical assay to screen for small mo... 来源：University of Pittsburgh Molecular Library Screening Center 靶标：furin (paired basic amino acid cleaving enzyme), isoform CRA_a [Homo sapiens] External Id：MH080376 Biochemical HTS for Inhibitors of the Proprotein Convertase Furin.

实验名称：Fluorescence polarization to screen for inhibitor that competite the binding of FadD2... 来源：Broad Institute 靶标：FATTY-ACID-CoA LIGASE FADD28 (FATTY-ACID-CoA SYNTHETASE) External Id：2147-01_Inhibitor_SinglePoint_HTS_Activity

实验名称：Bursicon-induced LGR2 mediated cAMP production in LGR-2/CRE6x-Luciferase co-transfect... 来源：Broad Institute 靶标：N/A External Id：Bursicon-induced LGR2 mediated cAMP production in LGR-2/CRE6x-Luciferase co-transfected HEK293 cells Inhibition - 7011-01_Antagonist_SinglePoint_HTS_Activity

实验名称：Primary Screen Inhibitors of CD40 Signaling in BL2 Cells Measured in Cell-Based Syste... 来源：Broad Institute 靶标：N/A External Id：7124-01_Inhibitor_SinglePoint_HTS_Activity

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δ-Secretaseinhibitor11英文别名

• 7-(Methylthio)xanthone-3-carboxamide
• 9H-Xanthene-3-carboxamide,7-(methylthio)-9-oxo
• 7-(morpholin-4-yl)-2,1,3-benzoxadiazol-4-amine