LY288513

• 常用名: LY288513
• 英文名: LY 288513
• CAS号: 147523-65-7
• 分子量: 436.30100
• 密度: 1.476g/cm3
• 沸点: N/A
• 分子式: C₂₂H₁₈BrN₃O₂
• 熔点: N/A
• 闪点: N/A

LY288513用途

LY288513,一种选择性非肽CCK-B受体拮抗剂,IC50值为16 nM。LY288513同时具有抗焦虑和抗精神病的潜力[1][2][3]。

LY288513名称

• 英文名: LY 288513,(4S,5R)-N-(4-Bromophenyl)-3-oxo-4,5-diphenyl-1-pyrazolidinecarboxamide

LY288513生物活性

• 描述: LY288513,一种选择性非肽CCK-B受体拮抗剂,IC50值为16 nM。LY288513同时具有抗焦虑和抗精神病的潜力[1][2][3]。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 胆囊收缩素受体
  研究领域 >> 神经疾病
• 靶点实验:

  IC50: 16 nM (CCK-B receptor)[1]

• 体外研究: LY288513(10纳米；2天)抑制CCK-8对CD4+T细胞亚群特异性转录因子的影响[2]。RT-PCR[2]细胞系：CD4+T细胞浓度：10nm孵育时间：2天结果：CCK-8抑制CD4+T细胞亚群特异性转录因子的作用。
• 体内研究: LY288513(3,10 mg/kg,腹腔注射；10,30 mg/kg,腹腔注射)产生抗焦虑作用[3]。LY288513(1000 mg/kg,p.o.)增强中枢神经系统抑制剂的作用,略微降低体温,仅在最高检查剂量下具有适度的镇静作用[3]。动物模型：雄性CD-l小鼠[3]剂量：3,10mg/kg；10,30mg/kg给药：腹腔注射。；p、 结果：在高强度脉冲中表现出抗焦虑作用。
• 参考文献:

  [1]. Rasmussen K. CCK, schizophrenia, and anxiety. CCK-B antagonists inhibit the activity of brain dopamine neurons. Ann N Y Acad Sci. 1994 Mar 23;713:300-11.

  [2]. Zhang JG, et al. Cholecystokinin octapeptide regulates the differentiation and effector cytokine production of CD4(+) T cells in vitro. Int Immunopharmacol. 2014;20(2):307-315.

  [3]. Helton DR, et al. Central nervous system characterization of the new cholecystokininB antagonist LY288513. Pharmacol Biochem Behav. 1996 Mar;53(3):493-502.

LY288513物理化学性质

• 密度: 1.476g/cm3
• 分子式: C₂₂H₁₈BrN₃O₂
• 分子量: 436.30100
• 精确质量: 435.05800
• PSA: 61.44000
• LogP: 5.19260
• InChIKey: LMUQHXHWJWQXSD-PMACEKPBSA-N
• SMILES: O=C1NN(C(=O)Nc2ccc(Br)cc2)C(c2ccccc2)C1c1ccccc1
• 折射率: 1.676

LY288513靶点实验

查看更多实验

实验名称：Discovery of Small Molecules to Inhibit Human Cytomegalovirus Nuclear Egress 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School 靶标：HCMV UL50 External Id：HMS1262

实验名称：Screen for inhibitors of RMI FANCM (MM2) intereaction 来源：11908 靶标：N/A External Id：RMI-FANCM-MM2

实验名称：Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VER... 来源：ChEMBL 靶标：Severe acute respiratory syndrome coronavirus 2 External Id：CHEMBL4513082

实验名称：Rescue cell viability in cybrid cells with a genetic mutation in complex 1 of the mit... 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School 靶标：N/A External Id：HMS1315

实验名称：Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Cac... 来源：ChEMBL 靶标：Severe acute respiratory syndrome coronavirus 2 External Id：CHEMBL4303805

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：SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response f... 来源：ChEMBL 靶标：Replicase polyprotein 1ab External Id：CHEMBL4495582

实验名称：Tocris HTS for Inhibitors of Aerobactin Synthetase lucA 来源：23265 External Id：IucA Pilot Assay Tocris Library

实验名称：A screen for compounds that inhibit viral RNA polymerase binding and polymerization a... 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School 靶标：Chain A, Poliovirus Polymerase With Gtp External Id：HMS750

实验名称：Enzymatic assay of human HDAC6 with commercial peptide substrate 来源：ChEMBL 靶标：Histone deacetylase 6 External Id：CHEMBL4808149

共17条，当前第1页，共2页

1

2