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抑制剂&激动剂
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  • 抑制剂&激动剂
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    抑制剂&激动剂
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    天然产物
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  • XE 991 dihydrochloride
    T17262122955-13-9
    XE 991 dihydrochloride 是有效的 Kv7 (KCNQ)通道阻滞剂,抑制 Kv7.1 (KCNQ1),Kv7.2 (KCNQ2),Kv7.2 + Kv7.3 (KCNQ3)通道以及 M-current,IC50分别为 0.75 µM、0.71 µM、0.6 μM、0.98 µM。
    • ¥ 403
    现货
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  • AM-92016 hydrochloride
    T5585133229-11-5
    AM-92016 hydrochloride 是一种整流钾电流的特异性阻断剂。它能够延迟整流钾通道,使膜复极化,限制神经冲动的持续时间。
    • ¥ 203
    现货
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    TargetMol | Inhibitor Sale
  • Dronedarone
    决奈达隆, SR 33589
    T7056141626-36-0
    Dronedarone (SR 33589) 是一种胺碘酮类似物,对治疗心房颤动可能有效。它是CYP3A4的底物和中度抑制剂。它是多种离子电流的有效阻滞剂,通过非竞争性结合到肾上腺素能受体显示出抗肾上腺素能的效果。
    • ¥ 119
    现货
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    TargetMol | Citations 客户已引用
  • XE991
    T78570122955-42-4In house
    XE991 是一种新型具有选择性的 Kv7 (KCNQ)通道阻滞剂。XE 991 抑制 Kv7.1 (KCNQ1)、Kv7.2 (KCNQ2)、Kv7.2 + Kv7.3 (KCNQ3)通道及M-current,可用于研究神经系统疾病。
    • ¥ 446
    现货
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    TargetMol | Citations 客户已引用
  • Linopirdine
    利诺吡啶, DuP 996
    T15758105431-72-9
    Linopirdine (DuP 996) 是一种口服有效的,选择性 M 型 K+电流 (IM;Kv7;KCNQ Channels) 抑制剂,IC50为 2.4 μM。Linopirdine 是TRPV1激活剂。Linopirdine 是一种公认的认知增强药物,可增加大鼠脑组织中乙酰胆碱的释放。
    • ¥ 313
    现货
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  • o-3M3FBS
    T23101313981-55-4
    o-3M3FBS 是 m-3M3FBS 的阴性对照。它以独立于 PLC 的机制及拮抗方式抑制内向和外向电流。它以与 m-3M3FBS 竞争的方式增加 [Ca2+]i 增加。
    • ¥ 233
    现货
    规格
    数量
  • 17R(18S)-EpETE
    17(R),18(S)-EETeTr, (17R,18S)-Epoxyeicosatetraenoic acid
    T36215725246-18-4
    17R(18S)-EpETE 是一种 oxylipin,同时也是 eicosapentaenoic acid 的 cytochrome P450 代谢产物。17R(18S)-EpETE 可激活大电导钙激活钾离子(BKCa)通道,在 50 nM 条件下于 +60 mV 电位时使分离的大鼠脑动脉血管平滑肌细胞中的钾电流振幅增加 15 倍。17R(18S)-EpETE 还可在新生大鼠心肌细胞中产生负性频率作用,EC50 约为 1–2 nM,并可抑制钙诱导的自发搏动增加。因此,17R(18S)-EpETE 被用于心血管电生理研究体系,以研究细胞模型中的离子通道调控、脂质介质信号以及心脏兴奋性调节。
    • ¥ 2230
    35日内发货
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  • Zonisamide-13C2,15N
    Zonisamide-13C2,15N
    T378471188265-58-8
    Zonisamide-13C2,15N is intended for use as an internal standard for the quantification of zonisamide by GC- or LC-MS. Zonisamide (T0267) is an antiepileptic agent.1 It selectively inhibits the repeated firing of sodium channels (IC50 = 2 μg/ml)in mouse embryo spinal cord neurons and inhibits spontaneous channel firing when used at concentrations greater than 10 μg/ml.2 In rat cerebral cortex neurons,zonisamide (1-1,000 μM)inhibits T-type calcium channels with a maximum reduction of 60% of the calcium current.3 Zonisamide (T0267)inhibits H. pylori recombinant carbonic anhydrase (CA)and the human CA isoforms I,II,and V with Ki values of 218,56,35,and 21 nM,respectively.4,5 In mice,it has anticonvulsant activity against maximal electroshock seizure (MES)and pentylenetetrazole-induced maximal,but not minimal,seizures (ED50s = 19.6,9.3,and >500 mg/kg,respectively). Zonisamide (T0267) (40 mg/kg,p.o.)prevents MPTP-induced decreases in the levels of dopamine ,but not homovanillic acid or dihydroxyphenyl acetic acid ,and increases MPTP-induced decreases in the dopamine turnover rate in mouse striatum in a model of Parkinson's disease.6 Formulations containing zonisamide have been used in the treatment of partial seizures in adults with epilepsy.
    • ¥ 6930
    35日内发货
    规格
    数量
  • Eltoprazine
    T3814598224-03-4
    Eltoprazine(DU28853) is a serenic or antiaggressive agent which as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor.IC50 value:Target: 5-HT1A/1B agonist; 5-HT2C antagonistin vitro: The binding of [3H]eltoprazine to whole tissue sections was saturable and revealed an apparent dissociation constant (Kd) of 11 nM. Specific [3H]eltoprazine binding was completely displaced by 5-HT; conversely, unlabelled eltoprazine reduced [3H]5-HT binding to the levels of non-specific binding [1]. Eltoprazine evoked membrane changes that were similar to but much weaker than those induced by 5HT. Both the 5HT- and eltoprazine-evoked membrane hyperpolarizations were largely suppressed in the presence of spiperone [2].in vivo: eltoprazine is extremely effective in suppressing dyskinesia in experimental models, although this effect was accompanied by a partial worsening of the therapeutic effect of l-dopa. Interestingly, eltoprazine was found to (synergistically) potentiate the antidyskinetic effect of amantadine. The current data indicated that eltoprazine is highly effective in counteracting dyskinesia in preclinical models [3]. Rats were chronically treated with mianserin (10 mg/kg i.p.) or eltoprazine (1 mg/kg i.p.) and were tested in the elevated plus-maze test for anxiety. Mianserin and eltoprazine displayed opposite effects in the elevated plus-maze: mianserin induced anxiolytic-like effects, while eltoprazine showed anxiogenic-like ones [4]. [1]. Sijbesma H, et al. Eltoprazine, a drug which reduces aggressive behaviour, binds selectively to 5-HT1 receptor sites in the rat brain: an autoradiographic study. Eur J Pharmacol. 1990 Feb 20;177(1-2):55-66. [2]. Joels M, et al. Eltoprazine suppresses hyperpolarizing responses to serotonin in rat hippocampus. J Pharmacol Exp Ther. 1990 Apr;253(1):284-9. [3]. Bezard E, et al. Study of the antidyskinetic effect of eltoprazine in animal models of levodopa-induced dyskinesia. Mov Disord. 2013 Jul;28(8):1088-96. [4]. Rocha B, et al. Chronic mianserin or eltoprazine treatment in rats: effects on the elevated plus-maze test and on limbic 5-HT2C receptor levels. Eur J Pharmacol. 1994 Sep 1;262(1-2):125-31.
    • ¥ 10600
    1-2周
    规格
    数量
  • Chlorahololide C
    TN36361007859-25-7
    Chlorahololide C is a potent and selective potassium channel blocker, it exerts potent and selective inhibition on the delayed rectifier (I(K)) K(+) current with the IC(50) value of 3.6 +/- 10.1 mu M.
    • ¥ 4280
    待询
    规格
    数量
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