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DREADD agonist 21

CAS No. 56296-18-5

DREADD agonist 21 ( —— )

产品货号. M26175 CAS No. 56296-18-5

DREADD agonist 21 is a potent agonist of human muscarinic acetylcholine M3 receptors (EC50=1.7 nM).

纯度: >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
2MG ¥381 有现货
5MG ¥721 有现货
10MG ¥1037 有现货
25MG ¥1936 有现货
50MG ¥3151 有现货
100MG ¥4690 有现货
200MG 获取报价 有现货
500MG 获取报价 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    DREADD agonist 21
  • 注意事项
    本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
  • 产品简述
    DREADD agonist 21 is a potent agonist of human muscarinic acetylcholine M3 receptors (EC50=1.7 nM).
  • 产品描述
    DREADD agonist 21 is a potent agonist of human muscarinic acetylcholine M3 receptors (EC50=1.7 nM).(In Vitro):DREADD agonist 21 is a highly selective and potent agonist for muscarinic DREADDs (pEC50 for hM1Dq=6.54 and that for hM4Di=7.77 in pERK assays). DREADD agonist 21 potently activates hM3Dq in Chinese hamster ovary (CHO) cells transfected cells in vitro (pEC50: 8.48±0.05) and it also potently activates hM1Dq, hM3Dq, and hM4Di. DREADD agonist 21 does not activate human M3 receptor (hM3). DREADD agonist 21 displays high binding affinities to 5HT2A and 5HT2C serotonin receptor, α1A adrenergic receptor, and H1 histamine receptor with Ki values of 66, 170, 280, and 6 nM, respectively. In addition to being inactive at hM3, DREADD agonist 21, a potent full agonist of hM3Dq (EC50=1.7 nM), is only 3.5-fold selective for hM3Dq over H1, 40-fold selective over 5HT2A, 100-fold selective over 5HT2C, and 165-fold selective over α1A. DREADD agonist 21 binds to hM1, hM4, hM1Dq and hM4Di receptors (pKis of 5.97, 5.44, 7.20, and 6.75, respectively). (In Vivo):DREADD agonist 21 has excellent pharmacokinetic properties, bioavailability and brain penetrability. DREADD agonist 21 (0.3, 1.0, and 3.0 mg/kg; i.p.) activates neuronal hM3Dq in mice. DREADD agonist 21 (0.1, 1, and 10 mg/kg; i.p.) shows 95.1% plasma protein binding and 95% brain protein bounding in mice.
  • 同义词
    ——
  • 通路
    Endocrinology/Hormones
  • 靶点
    5-HT Receptor
  • 受体
    Nuclear receptor NOT
  • 研究领域
    ——
  • 适应症
    ——

化学信息

  • CAS Number
    56296-18-5
  • 分子量
    278.4
  • 分子式
    C17H18N4
  • 纯度
    >98% (HPLC)
  • 溶解度
    ——
  • SMILES
    C1CN(CCN1)C1=Nc2ccccc2Nc2ccccc12
  • 化学全称
    ——

运输与储存

  • 储存条件
    (-20℃)
  • 运输条件
    With Ice Pack
  • 稳定性
    ≥ 2 years

参考文献

1.A Almario Garcia, P Lardenois, A Olivier. 2-ARYL-6-PHENYLIMIDAZO[1,2-α]PYRIDINE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF:WO, WO2008034974 A1.
产品手册
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