AVN-492

    
99%

AVN-492

源叶(MedMol)
S82408 一键复制产品信息
1220646-23-0
C17H21N5O2S
359.44594
货号 规格 价格 上海 北京 武汉 南京 购买数量
S82408-1mg 99% ¥280.00 10 - - -
S82408-5mg 99% ¥400.00 10 - - -
S82408-10mg 99% ¥680.00 9 - - -
S82408-50mg 99% ¥1280.00 7 - - -
S82408-100mg 99% ¥2400.00 货期:2-3天 - - -
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

AVN-492 is a very specific and highly-selective antagonist with picomolar affinity to 5-HT6R (Ki=91 pM)

产品描述: AVN-492 is a very specific and highly-selective antagonist with picomolar affinity to 5-HT6R (Ki=91 pM)
靶点: 5-HT6 Receptor:91 pM (Ki);5-HTReceptor
体外研究: The affinity of AVN-492 to bind to 5-HT6R (Ki=91 pM) is more than three orders of magnitude higher than that to bind to the only other target, 5-HT2BR, (Ki=170 nM). Thus, AVN-492 displays great 5-HT6R selectivity against all other serotonin receptor subtypes, and is extremely specific against any other receptors such as adrenergic, GABAergic, dopaminergic, histaminergic, etc
体内研究: In rats, the plasma, brain, and CSF concentrations of the PO administered AVN-492 are dose-dependent. The drug concentration curves for the plasma and brain are of hyperbolic shape and at all doses the brain-plasma ratio is near 11%. The drug concentration in CSF, however, is nearly linearly dependent on the dose, reaching 50% of the plasma level at 10mg/kg. In mice, the plasma and brain concentrations of AVN-492, given IV at a dose of 2 mg/kg, decreased with time but at both time points, 15 min and 60 min, the brain/plasma ratio (mean±SEM) is nearly the same, at 13.2±0.7% and 9.0±1.5%, respectively. This indicates that the steady-state concentration gradient of AVN-492 is established by at least 15 min after the drug administration
参考文献: 1. Ivachtchenko AV, et al. AVN-492, A Novel Highly Selective 5-HT6R Antagonist: Preclinical Evaluation. J Alzheimers Dis. 2017;58(4):1043-1063.
溶解性: soluble  in  DMSO
保存条件: -20℃
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 2.782 ml 13.91 ml 27.821 ml
5 mM 0.556 ml 2.782 ml 5.564 ml
10 mM 0.278 ml 1.391 ml 2.782 ml
50 mM 0.056 ml 0.278 ml 0.556 ml
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参考文献

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