| 中文名称: | A-740003 | ||||
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| 英文名称: | A-740003 | ||||
| 别名: | A-740003 N-(1-{[(cyanoimino)(5-quinolinylamino) methyl] amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide | ||||
| CAS No: | 861393-28-4 | 分子式: | C26H30N6O3 | 分子量: | 474.55 |
| CAS No: | 861393-28-4 | ||||
| 分子式: | C26H30N6O3 | ||||
| 分子量: | 474.55 | ||||
基本信息
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产品编号： |
A12326 |
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产品名称： |
A-740003 |
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CAS: |
861393-28-4 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
6个月 |
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分子量： |
474.55 |
-20℃ |
1个月 |
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化学名： |
N-(1-{[(cyanoimino)(5-quinolinylamino) methyl] amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide |
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Solubility (25°C)： |
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体外:
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DMSO |
95mg/mL (200.18mM) |
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Ethanol |
1.5mg/mL (3.16mM) |
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Water |
Insoluble |
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体内(现配现用): |
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。 请依序添加每种溶剂：10% DMSO 40% PEG300 5% Tween-80 45% saline Solubility:≥2.5mg/mL(5.27mM);Clear solution |
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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。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
2.1073mL |
10.5363mL |
21.0726mL |
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5mM |
0.4215mL |
2.1073mL |
4.2145mL |
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10mM |
0.2107mL |
1.0536mL |
2.1073mL |
生物活性
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产品描述 |
一种有效的，选择性的，竞争性的P2X7receptor拮抗剂，抑制大鼠和人的P2X7受体，IC50值分别为18和40nM。 |
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靶点 |
IC50:18nM (rat P2X7 receptor),40nM (human P2X7 receptor) |
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体外研究 |
A 438079 or A 740003 (10μM) significantly blocks the sustained phase of the BzATP-induced response.A-740003 infusion reduces SE-induced TNF-α expression in dentate granule cells.A-740003 infusions increases SE-induced neuronal death.A-740003 and A-438079 show significantly greater potency in blocking P2X7 receptor activation across all species compared with other antagonists.A-740003 and A-438079 show greater activity at rat and human,as compared with mouse P2X7 receptors.A-740003 potently blocks agonist-evoked IL-1β release with (IC50=156nM) and pore formation (IC50=92nM) in differentiated human THP-1 cells. |
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体内研究 |
Systemic administration of A-740003 produces dose-dependent antinociception in a spinal nerve ligation model (ED50=19mg/kg i.p.) in the rat.A-740003 also attenuates tactile allodynia in two other models of neuropathic pain,chronic constriction injury of the sciatic nerve and vincristine-induced neuropathy.In addition,A-740003 effectively reduces thermal hyperalgesia observed following intraplantar administration of carrageenan or complete Freund's adjuvant (ED50=38-54mg/kg i.p.).A-740003 is ineffective in attenuating acute thermal nociception in normal rats and does not alter motor performance at analgesic doses. |
推荐实验方法(仅供参考)
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动物实验: |
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The response to acute thermal stimulation is determined using a commercially available paw thermal stimulator.Rats are placed individually in Plexiglas cubicles mounted on a glass surface maintained at 30℃ and allowed a 30-min habituation period.A thermal stimulus,in the form of radiant heat emitted from a focused projection bulb,is then applied to the plantar surface of each hind paw.In each test session,each rat is tested in three sequential trials at approximately 5-min intervals.Paw-withdrawal latencies (PWLs) are calculated as the median of the two shortest latencies.An assay cut off is set at 20.5s.A-740003 is injected i.p.30 min before testing for acute thermal pain. |
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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 )
