中文名称: | AP521 | ||||
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英文名称: | AP521 | ||||
CAS No: | 151227-08-6 | 分子式: | C20H19ClN2O3S | 分子量: | 402.89 |
CAS No: | 151227-08-6 | ||||
分子式: | C20H19ClN2O3S | ||||
分子量: | 402.89 |
基本信息
产品编号: |
A11422 |
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产品名称: |
AP521 |
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CAS: |
151227-08-6 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
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分子量 |
402.89 |
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化学名: |
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Solubility (25°C): |
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体外:
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DMSO |
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Ethanol |
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Water |
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体内(现配现用): |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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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。 |
生物活性
产品描述 |
一种Hedgehog通路抑制剂。 |
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靶点 |
HT1A Receptor 94nM (IC50, in human) |
5-HT1A Receptor 135nM (IC50, in rat) |
HT1B Receptor 254nM (IC50, in rat) |
5-HT1B Receptor 5530nM (IC50, in human) |
HT1D Receptor 418nM (IC50, in human) |
HT5A Receptor 422nM (IC50, in human) |
5-HT7 Receptor 198nM (IC50, in rat) |
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体外研究 |
AP521 is an agonist of human 5-HT1A receptor with IC50s of 135, 94, 254, 5530, 418, 422 and 198nM for 5-HT1A (rat), 5-HT1A (human), 5-HT1B (rat), 5-HT1B (human), 5-HT1D (human), 5-HT5a (human) and 5-HT7 (rat), respectively. AP521 also decreases the forskolin-induced cAMP accumulation from 10nM to 10μM . |
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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 |
推荐实验方法(仅供参考)
Cell Assay |
Membranes of neurotransmitter receptors are prepared from the tissues of rat, mouse, and guinea pig or from recombinant cells. These membranes are incubated in assay buffers containing selective radioligand for each receptor and AP521. After the incubation, the mixture is vacuum filtered through a glass membrane filter and washed by cold reaction buffer. Afterward, the radioactivity of the filters is counted. |
Animal Administration |
Male Sprague-Dawley rats weighing 250 to 300 g are anesthetized with pentobarbital sodium (50 mg/kg, i.p.) and placed on a stereotaxic apparatus. Dialysis probes with an outer diameter of 0.105 mm are inserted into the guide cannulae so that 3.0mm of the probes are exposed to the tissue of the medial prefrontal cortex. Rats are housed individually after these operations. On the following day, perfusion is started in the home cage using artificial cerebrospinal fluid (145mM NaCl, 3.0mM KCl, 1.3mM CaCl2, 1.0mM MgCl2) at a flow rate of 2mL/min. AP521 (3, 10 mg/kg), tandospirone (10 mg/kg) or vehicle are administered subcutaneously 60 min after sample collection started. The dialysate samples are collected every 30 min for 180 min and extracellular levels of 5-HT are determined. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )