UBP-282

• 常用名: UBP-282
• 英文名: UBP 282
• CAS号: 544697-47-4
• 分子量: 333.29600
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₅H₁₅N₃O₆
• 熔点: N/A
• 闪点: N/A

UBP-282用途

UBP-282 是一种有效的,选择性的和竞争性的 AMPA 和海藻酸酯 (kainate receptor) 受体拮抗剂。UBP-282 抑制 fDR-VRP 的 IC50 值为 10.3 μM,拮抗海藻酸酯对背根的去极化作用,pA2 值为 4.96。

UBP-282名称

• 英文名: UBP 282,(αS)-α-Amino-3-[(4-carboxyphenyl)methyl]-3,4-dihydro-2,4-dioxo-1(2H)-pyrimidinepropanoicacid

UBP-282生物活性

• 描述: UBP-282 是一种有效的,选择性的和竞争性的 AMPA 和海藻酸酯 (kainate receptor) 受体拮抗剂。UBP-282 抑制 fDR-VRP 的 IC50 值为 10.3 μM,拮抗海藻酸酯对背根的去极化作用,pA2 值为 4.96。
• 相关类别:
  信号通路 >> 神经信号通路 >> iGluR
  研究领域 >> 神经疾病
  信号通路 >> 跨膜转运 >> iGluR
• 靶点实验:

  IC50: 10.3 μM (fast component of the dorsal root-evoked ventral root potential (fDR-VRP))[1] pA2: 4.96 (Kainate<-induced depolarisations of dorsal roots)[1]

• 体外研究: UBP-282(3-CBW)对运动神经元上表达的NMDA、mGlu和kainate受体的AMPA-和GluR5具有选择性[1][2]。200μM浓度的UBP-282(3-CBW)阻断AMPA诱发的运动神经元去极化,而对等剂量NMDA和DHPG的反应相对不受影响。在200μM UBP-282(一种完全消除运动神经元AMPA诱发去极化和背根红藻氨酸诱发反应的浓度)存在下,海藻酸钠对运动神经元仍有明显的去极化作用[1]。
• 体内研究: 新生大鼠运动神经元UBP-282(3-CBW)(200μM)对AMPA的反应几乎完全消失,而对NMDA、kainate和DHPG的反应分别为对照组的101.6%、39.4%和110.5%。因此,UBP-282可用于从AMPA受体介导的红藻氨酸受体反应中分离出红藻氨酸受体[1]。
• 参考文献:

  [1]. Julia C A More, et al. The novel antagonist 3-CBW discriminates between kainate receptors expressed on neonatal rat motoneurones and those on dorsal root C-fibres. Br J Pharmacol. 2002 Dec;137(7):1125-33.

  [2]. Julia C A More, et al. Structural requirements for novel willardiine derivatives acting as AMPA and kainate receptor antagonists. Br J Pharmacol. 2003 Mar;138(6):1093-100.

UBP-282物理化学性质

• 分子式: C₁₅H₁₅N₃O₆
• 分子量: 333.29600
• 精确质量: 333.09600
• PSA: 144.62000

UBP-282靶点实验

查看更多实验

实验名称：Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident pro... 来源：NCGC 靶标：N/A External Id：SERCaMPGLuc-p1-antagonist

实验名称：Validation qHTS for agonist of cAMP-regulated guanine nucleotide exchange factor 3 (E... 来源：NCGC External Id：epac1-activator-v

实验名称：Validation qHTS for antagonist of cAMP-regulated guanine nucleotide exchange factor 3... 来源：NCGC External Id：epac1-inhibitor-v

实验名称：Validation qHTS for agonist of cAMP-regulated guanine nucleotide exchange factor 4 (E... 来源：NCGC External Id：epac2-activator-v2

实验名称：Validation qHTS for antagonist of cAMP-regulated guanine nucleotide exchange factor 4... 来源：NCGC External Id：epac2-inhibitor-v2

实验名称：qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in... 来源：NCGC 靶标：TDP1 protein [Homo sapiens] External Id：TDP1100

实验名称：qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in... 来源：NCGC 靶标：TDP1 protein [Homo sapiens] External Id：TDP1101

实验名称：qHTS for Inhibitors of Polymerase Kappa 来源：NCGC 靶标：DNA polymerase kappa [Homo sapiens] External Id：PolK100

实验名称：Cell-based high throughput primary assay to identify activators of GPR151 来源：The Scripps Research Institute Molecular Screening Center 靶标：RecName: Full=G-protein coupled receptor 151; AltName: Full=G-protein coupled receptor PGR7; AltName: Full=GPCR-2037; AltName: Full=Galanin receptor 4; AltName: Full=Galanin-receptor-like protein; Short=GalRL External Id：GPR151_PHUNTER_AG_LUMI_1536_1X%ACT

实验名称：Antagonism on GLUK5 containing kainate induced depolarization of isolated neonatal ra... 来源：ChEMBL 靶标：Glutamate receptor ionotropic, kainate 1 External Id：CHEMBL862719

共23条，当前第1页，共3页

1

2

3

UBP-282英文别名

• ubp 282