Cyclo(his-pro)

• 常用名: Cyclo(his-pro)
• 英文名: Cyclo(-His-Pro)
• CAS号: 53109-32-3
• 分子量: 234.25400
• 密度: 1.36g/cm3
• 沸点: 650.3ºC at 760mmHg
• 分子式: C₁₁H₁₄N₄O₂
• 熔点: N/A
• 闪点: 347.1ºC

Cyclo(his-pro)用途

Cyclo(His-Pro)是结构上与促炎素释放激素相关的环状二肽。Cyclo(His-Pro) 可抑制 NF-κB 的核积聚。

Cyclo(his-pro)名称

• 中文名: 环(他-PRO)
• 英文名: 3-(1H-imidazol-5-ylmethyl)-2,3,6,7,8,8a-hexahydropyrrolo[1,2-a]pyrazine-1,4-dione

Cyclo(his-pro)生物活性

• 描述: Cyclo(His-Pro)是结构上与促炎素释放激素相关的环状二肽。Cyclo(His-Pro) 可抑制 NF-κB 的核积聚。
• 相关类别:
  多肽产品
  研究领域 >> 神经疾病
  天然产物 >> 其他
• 靶点实验:

  NF-κB

  Human Endogenous Metabolite

• 体外研究: Cyclo(His-Pro)是一种环状二肽,衍生自水解除去下丘脑促甲状腺激素释放激素的氨基末端焦谷氨酸残基。 Cyclo(His-Pro)在中枢神经系统中无处不在,是有机阳离子转运蛋白的关键底物,与神经保护密切相关。环状二肽也可以穿过脑血屏障,一旦进入大脑,就可以通过修饰Nrf2-NF-κB信号轴来影响不同的炎症和应激反应[1]。 Cyclo(His-Pro)通过Nrf2 /血红素加氧酶-1途径抑制百草枯在大鼠嗜铬细胞瘤PC12细胞中诱导的NF-κB核积累[2]。
• 体内研究: 接受环(His-Pro)预处理的小鼠显示出血管生成反应的显着降低,证实环状二肽可以发挥抗炎作用[2]。 Cyclo(His-Pro)通过下调肝和脑TNFα表达在中枢神经系统中发挥体内抗炎作用,从而抵抗LPS诱导的神经胶质增生。此外,通过上调Bip,环(His-Pro)增加ER应激敏感性并触发未折叠蛋白反应以减轻ER应激[3]。
• 细胞实验: 将永生化的小鼠小胶质细胞BV2细胞与50μM环（His-Pro）一起温育24小时，然后暴露于IL-6（5ng / mL）24小时。通过血细胞计数器计数活细胞，并且在用PBS洗涤细胞后通过常规MTT还原测定法评估活力[2]。
• 动物实验: 小鼠：Cyclo（His-Pro）抗炎作用通过在TPA之前30分钟在第二组（30只C57BL / 6小鼠）的右耳上局部施用1.8mg /耳环（His-Pro）来确定。在通过微米诱导炎症反应之前和之后测量耳厚度[2]。
• 参考文献:

  [1]. Grottelli S, et al. The Role of Cyclo(His-Pro) in Neurodegeneration. Int J Mol Sci. 2016 Aug 12;17(8). pii: E1332.

  [2]. Minelli A, et al. Cyclo(His-Pro) exerts anti-inflammatory effects by modulating NF-κB and Nrf2 signalling. Int J Biochem Cell Biol. 2012 Mar;44(3):525-35.

  [3]. Bellezza I, et al. Neuroinflammation and endoplasmic reticulum stress are coregulated by cyclo(His-Pro) to prevent LPS neurotoxicity. Int J Biochem Cell Biol. 2014 Jun;51:159-69.

Cyclo(his-pro)物理化学性质

• 密度: 1.36g/cm3
• 沸点: 650.3ºC at 760mmHg
• 分子式: C₁₁H₁₄N₄O₂
• 分子量: 234.25400
• 闪点: 347.1ºC
• 精确质量: 234.11200
• PSA: 78.09000
• InChIKey: NAKUGCPAQTUSBE-IUCAKERBSA-N
• SMILES: O=C1NC(Cc2cnc[nH]2)C(=O)N2CCCC12
• 储存条件: -20°C

Cyclo(his-pro)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：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：Flow Cytometric HTS Screen for inhibitors of the ABC transporter ABCB6 for Validation... 来源：NMMLSC 靶标：ATP-binding cassette sub-family B member 6, mitochondrial [Homo sapiens] External Id：UNMCMD_ABCB6_1o_ValidationSet

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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Cyclo(his-pro)英文别名

• cyclo-His-Pro
• Histidylproline dioxopiperazine
• Cyclo(his-pro)