KSK68

• 常用名: KSK68
• 英文名: KSK68
• CAS号: 2566715-91-9
• 分子量: 364.48
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₃H₂₈N₂O₂
• 熔点: N/A
• 闪点: N/A

KSK68用途

KSK68是一种高亲和力的双重sigma-1和组胺H3受体拮抗剂,H3受体、sigma-1、sigma-2受体的Kis分别为7.7、3.6、22.4 nM。KSK68对其他组胺受体亚型具有可忽略的亲和力。KSK68可用于伤害性疼痛和神经性疼痛的研究[1]。

KSK68名称

• 英文名: KSK68

KSK68生物活性

• 描述: KSK68是一种高亲和力的双重sigma-1和组胺H3受体拮抗剂,H3受体、sigma-1、sigma-2受体的Kis分别为7.7、3.6、22.4 nM。KSK68对其他组胺受体亚型具有可忽略的亲和力。KSK68可用于伤害性疼痛和神经性疼痛的研究[1]。
• 相关类别:
  信号通路 >> 免疫及炎症 >> 组胺受体
  研究领域 >> 神经疾病
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> Sigma Receptor
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体
• 靶点实验:

  7.7 nM, 3.6 nM、22.4 nM (H3 receptor, sigma-1, sigma-2 receptor)[1]

• 参考文献:

  [1]. Szczepańska K, et al. Dual Piperidine-Based Histamine H3 and Sigma-1 Receptor Ligands in the Treatment of Nociceptive and Neuropathic Pain. J Med Chem. 2023 Jul 27;66(14):9658-9683.

KSK68物理化学性质

• 分子式: C₂₃H₂₈N₂O₂
• 分子量: 364.48
• InChIKey: XFNQPNJGEZOKCM-UHFFFAOYSA-N
• SMILES: O=C(c1ccc(OCCCN2CCC(c3ccncc3)CC2)cc1)C1CC1

KSK68靶点实验

查看更多实验

实验名称：Antagonist activity at recombinant human H3R expressed in CHO-K1 cells assessed as re... 来源：ChEMBL 靶标：Histamine H3 receptor External Id：CHEMBL4734918

实验名称：Agonist activity at recombinant human H3R expressed in CHO-K1 cells assessed as inhib... 来源：ChEMBL 靶标：Histamine H3 receptor External Id：CHEMBL4734919

实验名称：Displacement of [3H]Nalpha-methylhistamine from recombinant human histamine H3 recept... 来源：ChEMBL 靶标：Histamine H3 receptor External Id：CHEMBL5350655

实验名称：Antagonist activity at recombinant human H3R expressed in CHO-K1 cells assessed as re... 来源：ChEMBL 靶标：Histamine H3 receptor External Id：CHEMBL4734917

实验名称：Displacement of [3H]DTG from sigma 2 receptor in Sprague-Dawley rat liver assessed as... 来源：ChEMBL 靶标：Sigma intracellular receptor 2 External Id：CHEMBL5350656

实验名称：Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membran... 来源：ChEMBL 靶标：Sigma non-opioid intracellular receptor 1 External Id：CHEMBL5350654

实验名称：Displacement of [3H]UR-PI294 from human SP-FLAG-tagged H3R expressed in HEK293T cells... 来源：ChEMBL 靶标：Histamine H3 receptor External Id：CHEMBL4734922

实验名称：Displacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expr... 来源：ChEMBL 靶标：Histamine H1 receptor External Id：CHEMBL4734923

实验名称：Antagonist activity at recombinant human H3R expressed in CHO-K1 cells assessed as in... 来源：ChEMBL 靶标：Histamine H3 receptor External Id：CHEMBL4734920

实验名称：Inhibition of recombinant CYP3A4 (unknown origin) at 10 uM measured after 30 mins by ... 来源：ChEMBL 靶标：Cytochrome P450 3A4 External Id：CHEMBL4734921

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