AVN-492|cas:1220646-23-0|西域试剂

AVN-492,99.49%

产品编号：Bellancom-101924| CAS NO：1220646-23-0| 分子式：C₁₇H₂₁N₅O₂S| 分子量：359.45

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货号	价格	库存与货期
Bellancom-101924	￥2400.00	杭州北京（现货）
Bellancom-101924	￥3600.00	杭州北京（现货）
Bellancom-101924	￥7100.00	杭州北京（现货）
Bellancom-101924	￥9900.00	杭州北京（现货）
Bellancom-101924	￥14000.00	杭州北京（现货）

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AVN-492

产品介绍

AVN-492 是一种高特异性的选择性 5-HT6R 拮抗剂，对 5-HT6R 具有皮摩尔级亲和力，K_i 为 91 pM。

生物活性

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

体外研究

The affinity of AVN-492 to bind to 5-HT6R (K_i=91 pM) is more than three orders of magnitude higher than that to bind to the only other target, 5-HT2BR, (K_i=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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (139.10 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7820 mL	13.9101 mL	27.8203 mL
5 mM	0.5564 mL	2.7820 mL	5.5641 mL
10 mM	0.2782 mL	1.3910 mL	2.7820 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 3.75 mg/mL (10.43 mM); Clear solution

此方案可获得 ≥ 3.75 mg/mL (10.43 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 37.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 3.75 mg/mL (10.43 mM); Clear solution

此方案可获得 ≥ 3.75 mg/mL (10.43 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 37.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。