PNU-120596

    
≥98%

N-(5-CHLORO-2,4-DIMETHOXYPHENYL)-N'-(5-METHYL-3-ISOXAZOLYL)-UREA

源叶(MedMol)
S47640 一键复制产品信息
501925-31-1
C13H14ClN3O4
311.72
MFCD00095313
PNU120596 , PNU 120596 , NSC 216666 , 化合物PNU120596 , PNU120596 PNU 120596 NSC 216666
货号 规格 价格 上海 北京 武汉 南京 购买数量
S47640-10mg ≥98% ¥330.00 10 - - -
S47640-50mg ≥98% ¥680.00 6 - - -
S47640-100mg ≥98% ¥1300.00 6 - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品

产品介绍

PNU-120596 (NSC 216666) is a potent and selective α7 nAChR positive allosteric modulator (PMA) with an EC50 of 216 nM. PNU-120596 is inactive against α4β2, α3β4, and α9α10 nAChRs. PNU-120596 has the potential for psychiatric and neurological disorders research

产品描述: PNU-120596 (NSC 216666) is a potent and selective α7 nAChR positive allosteric modulator (PMA) with an EC50 of 216 nM. PNU-120596 is inactive against α4β2, α3β4, and α9α10 nAChRs. PNU-120596 has the potential for psychiatric and neurological disorders research
靶点: EC50: 216 nM (α7 nAChR);AChR
体外研究: PNU-120596 increases agonist-evoked calcium flux mediated by an engineered variant of the human α7 nAChR. Electrophysiology studies confirme that PNU-120596 increases peak agonist-evoked currents mediated by wild-type receptors and also demonstrates a pronounced prolongation of the evoked response in the continued presence of agonist. PNU-120596 increases the channel mean open time of α7 nAChRs.
When applied to acute hippocampal slices, PNU-120596 increases the frequency of ACh-evoked GABAergic postsynaptic currents measured in pyramidal neurons.
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.
体内研究: PNU-120596 (1 mg/kg; intravenous injection; once) treatment improves the auditory gating deficit caused by Amphetamine in rats, a model proposed to reflect a circuit level disturbance associated with schizophrenia.
When administered before carrageenan, NU-120596 (30 mg/kg; i.p.) significantly reduces mechanical hyperalgesia and weight-bearing deficits for up to 4 h in Sprague-Dawley rats. PNU-120596 attenuates the carrageenan-induced increase in levels of TNF-α and IL-6 within the hind paw oedema Animal Model: Male Sprague Dawley rats (250-300 g) treated with Amphetamine Dosage: 1 mg/kg Administration: Intravenous injection; once Result: Improved the auditory gating deficit caused by Amphetamine.
细胞实验: Cell lines: MCF7 和 Ishikawa 细胞 Concentrations: 1000 nM Incubation Time: 8天 Method: MCF7和Ishikawa细胞在10%三倍活性炭处理的包含血清的培养基中生长3天。然后细胞以2,000细胞/孔的密度接种在96孔组织培养板,并按照指示每48小时处理一次。使用CellTiter-Glo发光细胞活性试剂盒根据制造商方案第一次处理后,第8天,进行细胞增殖试验
动物实验: Animal Models: 负荷 MCF-7 人乳腺肿瘤异种移植物的小鼠 Dosages: 8 mg/kg Administration: p.o.
参考文献: 1. Hurst RS, et al. A novel positive allosteric modulator of the alpha7 neuronal nicotinic acetylcholine receptor: in vitro and in vivo characterization. J Neurosci, 2005, 25(17), 4396-4405.
2. Barron SC, et al. An allosteric modulator of alpha7 nicotinic receptors, N-(5-Chloro-2,4-dimethoxyphenyl)-N'-(5-methyl-3-isoxazolyl)-urea (PNU-120596), causes conformational changes in the extracellular ligand binding domain similar to those caused by acetylcholine. Mol Pharmacol, 2009 76(2), 253-263.
3. Munro G, et al. The α7 nicotinic ACh receptor agonist compound B and positive allosteric modulator PNU-120596 both alleviate inflammatory hyperalgesia and cytokine release in the rat. Br J Pharmacol, 2012, doi: 10.1111/j.1476-5381.2012.02003.x
溶解性: Soluble  in  DMSO
保存条件: -20℃
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 3.208 ml 16.04 ml 32.08 ml
5 mM 0.642 ml 3.208 ml 6.416 ml
10 mM 0.321 ml 1.604 ml 3.208 ml
50 mM 0.064 ml 0.321 ml 0.642 ml
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