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Flupirtine maleate

CAS No. 75507-68-5

Flupirtine maleate ( D-9998 )

产品货号. M15872 CAS No. 75507-68-5

一种选择性神经元钾通道(KCNQ/KV7 通道)激活剂,还具有间接 NMDA 受体拮抗剂和 GABAA 受体调节特性。

纯度: >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
10MG ¥365 有现货
50MG ¥454 有现货
100MG ¥624 有现货
200MG ¥996 有现货
500MG ¥2398 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    Flupirtine maleate
  • 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
    一种选择性神经元钾通道(KCNQ/KV7 通道)激活剂,还具有间接 NMDA 受体拮抗剂和 GABAA 受体调节特性。
  • 产品描述
    A selective neuronal potassium channel (KCNQ/KV7 channel) activator that also has indirect NMDA receptor antagonist and GABAA receptor modulatory properties; a centrally acting non-opioid analgesic used as an analgesic for acute and chronic pain.Pain Discontinued(In Vitro):Flupirtine (0.1, 1, and 10 mM; 24 hours) significantly reduces the growth and viability of U373 malignant glioma cells with the GI50 of 0.47 mM. Flupirtine has neuroprotective effect of on U373 MG cells.Flupirtine Maleate is active at the KCNQ and GABAA channels in the range of 10-30 μM(In Vivo):Flupirtine (5 and 10 mg/kg) induces acute neuroprotection, reduces motor coordination impairment and ameliorates recombinant tissue plasminogen activator (rtPA)-induced toxicity.
  • 体外实验
    Flupirtine (0.1, 1, and 10 mM; 24 hours) significantly reduces the growth and viability of U373 malignant glioma cells with the GI50?of 0.47 mM. Flupirtine has neuroprotective effect of on U373 MG cells.Flupirtine Maleate is active at the KCNQ and GABAA?channels in the range of 10-30 μM.Cell Viability Assay Cell Line:U373 malignant glioma cell lines Concentration:0.001, 0.01, 0.1, 1, and 10 mM Incubation Time:24 hours Result:The growth of U373 MG cells was significantly reduced at high doses (1 and 10 mM) of flupirtine compared with low doses (0.001 to 0.1 mM) and control dose.
  • 体内实验
    Flupirtine (5 and 10 mg/kg) induces acute neuroprotection, reduces motor coordination impairment and ameliorates?recombinant tissue?plasminogen activator?(rtPA)-induced toxicity. Animal Model:Male C57BL6 mice (22-25 g each) Dosage:1, 5, 10 mg/kg Administration:Single intraperitoneal injection during post-ischemic reperfusion Result:Both 5 and 10 mg/kg reduced infarct volumes on day 2 post-stroke, no effect was observed with 1 mg/kg.?
  • 同义词
    D-9998
  • 通路
    Cell Cycle/DNA Damage
  • 靶点
    Potassium Channel
  • 受体
    NMDAreceptor|PotassiumChannel
  • 研究领域
    Neurological Disease
  • 适应症
    Pain

化学信息

  • CAS Number
    75507-68-5
  • 分子量
    420.3916
  • 分子式
    C19H21FN4O6
  • 纯度
    >98% (HPLC)
  • 溶解度
    DMSO: ≥ 40 mg/mL
  • SMILES
    CCOC(=O)NC1=C(N=C(C=C1)NCC2=CC=C(C=C2)F)N.C(=C\C(=O)O)\C(=O)O
  • 化学全称
    Carbamic acid, N-[2-amino-6-[[(4-fluorophenyl)methyl]amino]-3-pyridinyl]-, ethyl ester, (2Z)-2-butenedioate (1:1)

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. Szelenyi I, et al. Inflamm Res. 2013 Mar;62(3):251-8. 2. Harish S, et al. J Anaesthesiol Clin Pharmacol. 2012 Apr;28(2):172-7. 3. Hedegaard ER, et al. J Pharmacol Exp Ther. 2016 Apr;357(1):94-102.
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