N-(5-氯-2,4-二甲氧基苯基)-N'-(5-甲基-3-异唑基)脲

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发布时间： 2024-07-15 12:35:29

CAS号：501925-31-1

常用名： N-(5-氯-2,4-二甲氧基苯基)-N’-(5-甲基-3-异唑基)脲

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纯度： 98.0%

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用途： PNU-120596 (NSC 216666 ) is a potent and selective positive allosteric α7 nAChR modulator with an EC50 of 0.2 μM.IC50 value: 0.2 uM (EC50) [1] Target: α7in vitro: PNU-120596 increases agonist (Ach)-evoked calcium flux mediated by an engineered variant of the human α7 nAChR. PNU-120596 increases agonists (choline and ACh)-evoked currents mediated by wild-type receptors and also demonstrates a pronounced prolongation of the evoked response in the continued presence of agonist in Xenopus oocytes. PNU-120596 increases the channel mean open time ofα7 nAChRs but has no effect on ion selectivity and relatively little, if any, effect on unitary conductance. When applied to acute hippocampal slices, PNU-120596 increases the frequency of ACh-evoked GABAergic postsynaptic currents measured in pyramidal neurons; this effect is suppressed by TTX, suggesting that PNU-120596 modulates the function of α7 nAChRs located on the somatodendritic membrane of hippocampal interneurons [1]. Besides the positive modulation to α7 nAChR, PNU-120596 induces a profound retardation of the kinetics of desensitization, raising the potential of Ca2+-induced toxicity through excessive stimulation of α7 nAChR [2]. PNU-120596 causes changes in cysteine accessibility at the inner beta sheet, transition zone and agonist binding site while binding to α7 nAChR. Binding sites for PNU-120596 are not in the agonist-binding sites and PNU-120596 enhances agonist-evoked gating of nicotinic receptors by eliciting conformational effects that are similar but nonidentical to the gating conformations promoted by Ach [3].in vivo: Systemic administration of PNU-120596 (1 mg/kg) to rats improves the auditory gating deficit caused by amphetamine, a model proposed to reflect a circuit level disturbance associated with schizophrenia. [1] When administered prior to Carrageenan, 30 mg/kg PNU-1230596 significantly blunts mechanical hyperalgesia and weight bearing deficits for up to 4 hours. PNU-120596 attenuates the carrageenan-induced increase in levels of TNF-α and IL-6 within the hindpaw oedema, diclofenac only attenuated IL-6 levels. Established mechanical hyperalgesia induced by Carrageenan or CFA is also partially reversed by PNU-120596 [4]. 物理化学性质： CAS号：501925-31-1 常用中文名：N-(5-氯-2,4-二甲氧基苯基)-N’-(5-甲基-3-异唑基)脲常用英文名：PNU-120596 分子式：C13H14ClN3O4 分子量：311.721 密度：1.4±0.1 g/cm3 沸点：385.0±42.0 °C at 760 mmHg 熔点：N/A 闪点：186.6±27.9 °C 储存条件：Desiccate at +4°C

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2022-02-19 价格：￥426.9 PNU-120596

2024-07-15 价格：需询单 N-(5-氯-2,4-二甲氧基苯基)-N'-(5-甲基-3-异唑基)脲

2021-02-06 价格：￥6089.0 PNU-120596

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N-(5-氯-2,4-二甲氧基苯基)-N’-(5-甲基-3-异唑基)脲价格

N-(5-氯-2,4-二甲氧基苯基)-N'-(5-甲基-3-异唑基)脲

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