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现货,LY404039,selleck,美国进口,mGluR YZ剂,CAS号: 635318-11-5,目录号 S6001

产品信息
  • 规格: Kit 产品价格: ¥1323
    规格: 5mg 产品价格: ¥1323
    S6001 LY404039
    信号转导通路:  神经信号通路(Neuronal Signaling) >> mGluR >> mGluR YZ剂 >> 
    技术数据:
    S6001 LY404039
    信号转导通路:  神经信号通路(Neuronal Signaling) >> mGluR >> mGluR YZ剂 >> 
    技术数据:
    分子量(MW): 235.22
    化学式:

    C7H9NO6S

    溶解度: DMSO ≥1mg/mL   Water <1mg/mL   Ethanol <1mg/mL
    纯度: >99%
    稳定性: at -20℃ 2 years
    CAS号: 635318-11-5
    生物活性

     

    LY404039 is a selective metabotropic glutamate receptor group II subtypes mGluR2 and mGluR3 agonist with Ki of 149 and 92nM for mGlu2 and mGlu3, respectively.Functional activity of LY404039 at group II and group III mGlu receptors is measured by the inhibition of forskolin-stimulated cAMP formation. It is nanomolar potent agonists at human mGlu2 and mGlu3 receptors, as indicated by the inhibition of forskolin-stimulated cAMP formation (LY404039: mGlu2, EC50 =23 nM; mGlu3, EC50 = 48 nM). It suppressed the frequency of 5-HT-induced EPSCs with an EC50 of 82.3 nM and with a near maximal suppression of 85.6% at 1 μM. Intraperitoneal administration of LY404039 (10 mg/kg) to wild-type mice significantly inhibited increases evoked by PCP (7.5 mg/kg) in ambulations. It produced a dose-dependent reduction of increases evoked by AMP (5 mg/kg) in ambulations. [1][2]

     

    参考文献
    • Pharmacological and Pharmacokinetic Properties of a Structurally Novel, Potent, and Selective Metabotropic Glutamate 2/3 Receptor Agonist: In Vitro Characterization of Agonist (-)-(1R,4S,5S,6S)-4-Amino-2-sulfonylbicyclo[3.1.0]-hexane-4,6-dicarboxylic Acid (LY404039) Linda M. Rorick-Kehn, Bryan G. Johnson,et al. JPET 2007;321:308–317
    • Evidence for the Role of Metabotropic Glutamate (mGlu)2 Not mGlu3 Receptors in the Preclinical Antipsychotic Pharmacology of the mGlu2/3 Receptor Agonist (-)-(1R,4S,5S,6S)-4-Amino-2-sulfonylbicyclo[3.1.0]hexane-4,6-dicarboxylic Acid (LY404039) Matthew J. Fell, Kjell A. Svensson,et al. JPET 2008;326:209–217
    客户反馈数据

    Top: The glutamate agonist LY404039 inhibited the binding of 2 nM [3H]domperidone on dopamine D2Long receptors (in CHO cells). Bottom: LY404039 stimulated the incorporation of [35S]GTP-g-S into dopamine D2Long receptors with 50% incorporation occurring at 80 6 15 nM.

     
     

     

    如果需要长期保存,请于零下二十度低温保存。
    禁止用于人体及ZL!

    特定的存储和包装每个产品的信息在产品说明书上都有注明 。大多数Selleck产品,在推荐的条件下存储可稳定保存两年。产品有时建议的储存温度不同,大多数建议储存在-20 ° C ,抗体及蛋白等产品建议-60℃。YZ剂属于化学试剂,可在常温下运输储存两周左右。即使如此,我们保证产品的出货量将保持产品质量的条件下,一般都会放入冰袋。望阁下收到产品后,请按照产品数据表建议适当存储。 

    分子量(MW): 235.22
    化学式:

    C7H9NO6S

    溶解度: DMSO ≥1mg/mL   Water <1mg/mL   Ethanol <1mg/mL
    纯度: >99%
    稳定性: at -20℃ 2 years
    CAS号: 635318-11-5
    生物活性

     

    LY404039 is a selective metabotropic glutamate receptor group II subtypes mGluR2 and mGluR3 agonist with Ki of 149 and 92nM for mGlu2 and mGlu3, respectively.Functional activity of LY404039 at group II and group III mGlu receptors is measured by the inhibition of forskolin-stimulated cAMP formation. It is nanomolar potent agonists at human mGlu2 and mGlu3 receptors, as indicated by the inhibition of forskolin-stimulated cAMP formation (LY404039: mGlu2, EC50 =23 nM; mGlu3, EC50 = 48 nM). It suppressed the frequency of 5-HT-induced EPSCs with an EC50 of 82.3 nM and with a near maximal suppression of 85.6% at 1 μM. Intraperitoneal administration of LY404039 (10 mg/kg) to wild-type mice significantly inhibited increases evoked by PCP (7.5 mg/kg) in ambulations. It produced a dose-dependent reduction of increases evoked by AMP (5 mg/kg) in ambulations. [1][2]

     

    参考文献
    • Pharmacological and Pharmacokinetic Properties of a Structurally Novel, Potent, and Selective Metabotropic Glutamate 2/3 Receptor Agonist: In Vitro Characterization of Agonist (-)-(1R,4S,5S,6S)-4-Amino-2-sulfonylbicyclo[3.1.0]-hexane-4,6-dicarboxylic Acid (LY404039) Linda M. Rorick-Kehn, Bryan G. Johnson,et al. JPET 2007;321:308–317
    • Evidence for the Role of Metabotropic Glutamate (mGlu)2 Not mGlu3 Receptors in the Preclinical Antipsychotic Pharmacology of the mGlu2/3 Receptor Agonist (-)-(1R,4S,5S,6S)-4-Amino-2-sulfonylbicyclo[3.1.0]hexane-4,6-dicarboxylic Acid (LY404039) Matthew J. Fell, Kjell A. Svensson,et al. JPET 2008;326:209–217
    客户反馈数据

    Top: The glutamate agonist LY404039 inhibited the binding of 2 nM [3H]domperidone on dopamine D2Long receptors (in CHO cells). Bottom: LY404039 stimulated the incorporation of [35S]GTP-g-S into dopamine D2Long receptors with 50% incorporation occurring at 80 6 15 nM.

     
     

     

    如果需要长期保存,请于零下二十度低温保存。
    禁止用于人体及ZL!

    特定的存储和包装每个产品的信息在产品说明书上都有注明 。大多数Selleck产品,在推荐的条件下存储可稳定保存两年。产品有时建议的储存温度不同,大多数建议储存在-20 ° C ,抗体及蛋白等产品建议-60℃。YZ剂属于化学试剂,可在常温下运输储存两周左右。即使如此,我们保证产品的出货量将保持产品质量的条件下,一般都会放入冰袋。望阁下收到产品后,请按照产品数据表建议适当存储。

    温馨提示:不可用于临床ZL。
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