GR 89696 fumarate

• 常用名: GR 89696 fumarate
• 英文名: GR 89696 fumarate
• CAS号: 126766-32-3
• 分子量: 530.39800
• 密度: N/A
• 沸点: 559.2ºC at 760 mmHg
• 分子式: C₂₃H₂₉Cl₂N₃O₇
• 熔点: N/A
• 闪点: 292ºC

GR 89696 fumarate用途

GR 89696是一种高选择性κ2阿片受体激动剂,具有预防瘙痒的潜力[1]。

GR 89696 fumarate名称

• 英文名: GR 89696 fumarate,4-[(3,4-Dichlorophenyl)acetyl]-3-(1-pyrrolidinylmethyl)-1-piperazinecarboxylicacidmethylesterfumarate

GR 89696 fumarate生物活性

• 描述: GR 89696是一种高选择性κ2阿片受体激动剂,具有预防瘙痒的潜力[1]。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 阿片受体
  研究领域 >> 炎症/免疫
  信号通路 >> 神经信号通路 >> 阿片受体
• 体内研究: GR 89696(肌肉注射,0.01-0.1μg/kg)可以以一种剂量依赖的方式减轻鞘内注射吗啡(0.03mg)诱导的抓挠反应而不影响吗啡镇痛作用[1]。 GR-896960(皮下注射,1 mg/kg)在大鼠永久性局灶性缺血模型中,使大脑动脉梗塞体积减少了 38%[2]。
• 参考文献:

  [1]. Mei-Chuan Ko, et al. Effects of atypical kappa-opioid receptor agonists on intrathecal morphine-induced itch and analgesia in primates. J Pharmacol Exp Ther. 2009 Jan;328(1):193-200.

  [2]. A Barber, et al. Effects of GR-89696 and the novel peripherally selective OP2 agonists, EMD-61569 and EMD-61747, against focal cerebral ischemia in the rat. Methods Find Exp Clin Pharmacol. 1999 Mar;21(2):105-13

GR 89696 fumarate物理化学性质

• 沸点: 559.2ºC at 760 mmHg
• 分子式: C₂₃H₂₉Cl₂N₃O₇
• 分子量: 530.39800
• 闪点: 292ºC
• 精确质量: 529.13800
• PSA: 127.69000
• LogP: 2.43640
• InChIKey: ABTNETSDXZBJTE-WLHGVMLRSA-N
• SMILES: COC(=O)N1CCN(C(=O)Cc2ccc(Cl)c(Cl)c2)C(CN2CCCC2)C1.O=C(O)C=CC(=O)O
• 蒸汽压: 1.55E-12mmHg at 25°C

GR 89696 fumarate安全信息

• 个人防护装备: Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
• 危险品运输编码: NONH for all modes of transport

GR 89696 fumarate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：Thermal Shift Assay. Domain: start/stop: M1-L298 来源：ChEMBL 靶标：Cyclin-dependent kinase 2 External Id：CHEMBL5062802

实验名称：Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay 来源：ChEMBL 靶标：N/A External Id：CHEMBL1266185

实验名称：Thermal Shift Assay. Domain: start/stop: S229-K512 来源：ChEMBL 靶标：Tyrosine-protein kinase ABL1 External Id：CHEMBL5060754

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：Antibacterial activity against Staphylococcus aureus MRSA ATCC 43300 (CO-ADD:GP_020);... 来源：ChEMBL 靶标：Staphylococcus aureus External Id：CHEMBL4296184

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：Antibacterial activity against Klebsiella pneumoniae MDR ATCC 70063 (CO-ADD:GN_003); ... 来源：ChEMBL 靶标：Klebsiella pneumoniae External Id：CHEMBL4296186

实验名称：Antibacterial activity against Escherichia coli ATCC 25922 (CO-ADD:GN_001); MIC in CA... 来源：ChEMBL 靶标：Escherichia coli External Id：CHEMBL4296185

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

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