货号	规格	价格	上海	北京	珠海	重庆	武汉
S82408-1mg买3赠1	99.50%	￥270.00 S82408-1mg ￥270.00 现货（买3赠1）	9 9	-	-	-	-
S82408-5mg买3赠1	99.50%	￥400.00 S82408-5mg ￥400.00 现货（买3赠1）	9 9	-	-	-	-
S82408-10mg买3赠1	99.50%	￥680.00 S82408-10mg ￥680.00 现货（买3赠1）	8 8	-	-	-	-
S82408-50mg促销	99.50%	￥1280.00 ￥1020.00 S82408-50mg ￥1020.00 现货	6 6	-	-	-	-
S82408-100mg促销	≥99%	￥2400.00 ￥1920.00 S82408-100mg ￥1920.00 2-3天	0 货期：2-3天	-	-	-	-

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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

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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