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  • Luzindole

    • N-Acetyl-2-benzyltryptamine; N-[2-[2-(Phenylmethyl)-1H-indol-3-yl]ethyl]acetamide
    货号: abs819807
    CAS号: 117946-91-5
    分子式: C19H20N2O
    分子量: 292.37
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    货号-规格 货期 价格 数量
    abs819807-5mg 4周 ¥945.00
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    abs819807-25mg 4周 ¥3209.00
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    大包装询价
    产品描述
    描述

    Luzindole is a melatonin receptor antagonist, with a 25-fold higher affinity for the MEL-1B-R over the MEL-1A-R receptor subtype. Melatonin is a hormone produced endogenously from serotonin (5-HT), and melatonin interaction at the MEL-1B-R receptor is thought to represent a chemical underpinning for circadian rhythm and the sleep-wake cycle. Luzindole MEL-1B-R antagonism is described to modulate functions of melatonin signaling and the relationship between melatonin regulation and neurotransmission. Luzindole blocks melatonin-mediated inhibition of forskolin-stimulated cyclic AMP production in CHO cells. At 1μM Luzindole antagonizes the melatonin-elicited inhibition of calcium-dependent dopamine release, and at higher concentrations (from 1μM to 10μM) affects the response of this dopamine release mechanism to melatonin concentrations (shifts the dose-response curve). Melatonin activation of the MEL-1B-R receptor advances the circadian rhythm, and antagonism by Luzindole shows a similar shift in the dose-response curve for the response of biological timing to melatonin concentration, providing evidence that the MEL-1B-R receptor indeed represents a chemical foundation for the circadian timing system. Luzindole significantly antagonizes melatonin-mediated antinociception, suggesting that MEL-1B-R plays a further role as a mediator of melatonin modulation of pain signaling.

    纯度
    ≥98%
    储存/保存方法
    Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
    基本信息
    别名
    N-Acetyl-2-benzyltryptamine; N-[2-[2-(Phenylmethyl)-1H-indol-3-yl]ethyl]acetamide
    外观
    White to off-white crystalline solid
    熔点
    216.19° C (Predicted)
    折射率
    n20D 1.63 (Predicted)
    IC50
    melatonin-induced pigment aggregation : IC50 = 2.10 µM (frog); melatonin of Xenopus melanophores: IC50 = 2.46 µM (frog)
    Ki 数据
    MEL-1B-R: Ki= 44.7 nM (human); MEL-1A-R: Ki= 603 nM (human); Melatonin receptor: Ki= 1606 nM (Gallus gallus)
    可溶性/溶解性
    DMSO : 250 mg/mL (855.08 mM; Need ultrasonic)
    生物活性
    In vitro(体外研究)
    Luzindole (N-0774) (5-10 μg/ml) inhibits antigen-specific proliferation of the MBP-reactive LV-4 T cell line.
    In vivo(体内研究)
    Luzindole (N-0774) (30 mg/kg; i.p.; days 0-5) suppresses experimental autoimmune encephalomyelitis.
    温馨提示:本产品仅作科研实验使用,不支持临床等研究
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