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  3. HIT220912866
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HIT220912866
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HIT220912866
  • HIT ID:HIT220912866
  • Cas No:1310817-94-7
  • 常用名:RO-5328673
  • IUPAC:4-fluorophenyl N-[(3S,4R)-4-(3,4-dichlorophenyl)-1-[1-(1-methylcyclopropanecarbonyl)piperidine-4-carbonyl]pyrrolidin-3-yl]-N-methylcarbamate
    IUPAC:4-fluorophenyl N-[(3S,4R)-4-(3,4-dichlorophenyl)-1-[1-(1-methylcyclopropanecarbonyl)piperidine-4-carbonyl]pyrrolidin-3-yl]-N-methylcarbamate
  • InChI key:InChIKey=QQHBMXDSZDWXLY-WIOPSUGQSA-N
  • 分子式:C29H32Cl2FN3O4
  • 分子量:576.49
  • 氢键供体数 (HBD):
  • 氢键受体数 (HBA):
  • LogP:
  • SMILES:CN([C@@H]1CN(C[C@H]1c1ccc(Cl)c(Cl)c1)C(=O)C1CCN(CC1)C(=O)C1(C)CC1)C(=O)Oc1ccc(F)cc1
    SMILES:CN([C@@H]1CN(C[C@H]1c1ccc(Cl)c(Cl)c1)C(=O)C1CCN(CC1)C(=O)C1(C)CC1)C(=O)Oc1ccc(F)cc1
  • RO-5328673 is a dual NK2/NK3 antagonist. O5328673. [(3)H]RO5328673 bound to a single saturable site on hNK2, hNK3 and gpNK3 with high-affinity. RO5328673 acted as an insurmountable antagonist at both human and guinea-pig NK3 receptors in the [(3)H]IP accumulation assay. In binding kinetic analyses, [(3)H]RO5328673 had fast association and dissociation rates at hNK2 while it had a fast association rate and a remarkably slow dissociation rate at gp and hNK3. In electrophysiological recordings of gp SNpc, RO5328673 inhibited the senktide-induced potentiation of spontaneous activity of dopaminergic neurons with an insurmountable mechanism of action. RO5328673 exhibited in-vivo activity in gerbils, robustly reversing the senktide-induced locomotor activity.
市场产品/服务共显示1个结果
  • 供应商
    TargetMolSC
    规格
    货期
    8-10周
    纯度
    -
    ¥ 15,000.00
    1

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