AP521|cas:151227-08-6|西域试剂

AP521,98.96%

产品编号：Bellancom-100166| CAS NO：151227-08-6| 分子式：C₂₀H₁₉ClN₂O₃S| 分子量：402.89

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-100166		￥5800.00	杭州北京（现货）
Bellancom-100166		￥14500.00	杭州北京（现货）

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AP521

产品介绍

AP521 是一个人 5-HT_1A 受体激动剂，其 IC₅₀ 值为 94 nM。

生物活性

AP521 is an agonist of human 5-HT_1A receptor with an IC₅₀ of 94 nM.

体外研究

AP521 is an agonist of human 5-HT_1A receptor with IC₅₀s of 135, 94, 254, 5530, 418, 422 and 198 nM for 5-HT_1A (rat), 5-HT_1A (human), 5-HT_1B (rat), 5-HT_1B (human), 5-HT_1D (human), 5-HT_5a (human) and 5-HT₇ (rat), respectively. AP521 also decreases the forskolin-induced cAMP accumulation from 10 nM to 10 μM.

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

体内研究

AP521 significantly increases the number of shock acceptances [F(5,105)=4.46, P<0.01] at doses between 0.5 to 10 mg/kg. Oral administration of AP521 at 3 and 10 mg/kg significantly decreases freezing time [F(3,60)=2.89, P<0.05]. AP521 significantly increases the time spent on the open arms by approximately 2-fold as compare to the vehicle treated group [F(3, 36)=4.21, P<0.05 for AP521]. The anxiolytic-like effect of AP521 appears to be dose-related. AP521 significantly increases the extracellular 5-HT level of the medial prefrontal cortex (mPFC) at 10 mg/kg from 0.5 to 1 h after administration. AP521 at 3 mg/kg tends to increase the extracellular 5-HT level, however, this increase is not significant.

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 : 25 mg/mL (62.05 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4821 mL	12.4103 mL	24.8207 mL
5 mM	0.4964 mL	2.4821 mL	4.9641 mL
10 mM	0.2482 mL	1.2410 mL	2.4821 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 (sealed storage, away from moisture and light)。-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: ≥ 2.5 mg/mL (6.21 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.21 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.21 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.21 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明