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S86044

TBPB

MedMol 99%
  • 英文名:
  • TBPB
  • 別名:
  • CAS號:
  • 634616-95-8
  • 分子式:
  • C25H32N4O
  • 分子量:
  • 404.54778
  • 核磁/質譜:
品牌貨號產品規(guī)格價格(RMB) 庫存(上海) 北京 武漢 南京 數(shù)量計量單位 加入購物車...
MedMol S86044-5mg 99% ¥400.00元 5 - - - EA 加入購物車
MedMol S86044-10mg 99% ¥560.00元 5 - - - EA 加入購物車
MedMol S86044-25mg 99% ¥1120.00元 7 - - - EA 加入購物車
源葉(MedMol) S86044-100mg 99% ¥3200.00元 預計交期:2-3天 - - - EA 加入購物車
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  • 提示:詳情請下載說明書。
  • 產品描述: TBPB is an allosteric M1 mAChR agonist(EC50=289 nM) that regulates amyloid processing and produces antipsychotic-like activity in rats. IC50 value: 289 nM(EC50) Target: M1 mAChR agonist in vitro: TBPB activates M(1) through an allosteric site rather than the orthosteric acetylcholine binding site, which is likely critical for its unprecedented selectivity. Whole-cell patch-clamp recordings demonstrated that activation of M(1) by TBPB potentiates NMDA receptor currents in hippocampal pyramidal cells but does not alter excitatory or inhibitory synaptic transmission, responses thought to be mediated by M(2) and M(4) . in vivo: TBPB was efficacious in models predictive of antipsychotic-like activity in rats at doses that did not produce catalepsy or peripheral adverse effects of other mAChR agonists
  • 靶點: mAChR;AChR
  • 參考文獻:
    1. Jones CK, et al. Novel selective allosteric activator of the M1 muscarinic acetylcholine receptor regulates amyloid processing and produces antipsychotic-like activity in rats. J Neurosci. 2008 Oct 8;28(41):10422-33. 2. Miller NR, et al. Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas--the effect of capping the distal basic piperidine nitrogen. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5443-7.
  • 溶解性: soluble  in  DMSO
  • 保存條件: -20℃
  • 配置溶液濃度參考:
    1mg 5mg 10mg
    1 mM 2.472 ml 12.359 ml 24.719 ml
    5 mM 0.494 ml 2.472 ml 4.944 ml
    10 mM 0.247 ml 1.236 ml 2.472 ml
    50 mM 0.049 ml 0.247 ml 0.494 ml
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