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PA-8
很棒产品编号 T41005Cas号 878437-15-1
PA-8是一种小分子的的 PACAP I 型(PAC1)受体拮抗剂，有 选择性、有效性和口服活性。PA-8抑制PACAP 诱导的CREB 在PAC1-受体上的磷酸化，但对VPAC11或VPAC2受体无抑制作用。PA-8也抑制pacap 诱导的体外cAMP 水平升高(IC50 = 2 nM)和体内鞘内注射后pacap 诱导的厌恶反应和机械异位性痛。
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PA-8
很棒 纯度: 97.64%
产品编号 T41005Cas号 878437-15-1
PA-8是一种小分子的的 PACAP I 型(PAC1)受体拮抗剂，有 选择性、有效性和口服活性。PA-8抑制PACAP 诱导的CREB 在PAC1-受体上的磷酸化，但对VPAC11或VPAC2受体无抑制作用。PA-8也抑制pacap 诱导的体外cAMP 水平升高(IC50 = 2 nM)和体内鞘内注射后pacap 诱导的厌恶反应和机械异位性痛。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 185 | 现货 | |
| 5 mg | ¥ 413 | 现货 | |
| 10 mg | ¥ 747 | 现货 | |
| 25 mg | ¥ 1,570 | 现货 | |
| 50 mg | ¥ 2,730 | 现货 | |
| 100 mg | ¥ 4,130 | 现货 | |
| 1 mL x 10 mM (in DMSO) | ¥ 455 | 现货 |
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纯度:97.64%
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生物活性
化学信息
| 产品描述 | PA-8 is a small molecule receptor antagonist for PACAP Type I (PAC1) that is selective, effective, and orally active. PA-8 inhibits PacAP-induced CREB phosphorylation at PAC1- receptors, but does not inhibit VPAC1- or vpac2 receptors. PA-8 also inhibited PacAP-induced elevation of cAMP levels in vitro (IC50 = 2 nM) and PacAP-induced aversive response and mechanical atopic pain after intrathecal injection in vivo. |
| 靶点活性 | cAMP:2 nM |
| 体外活性 | 在PAC1/CHO细胞中，PA-8（10 pM至10 nM；30分钟）呈剂量依赖性抑制PACAP（1 nM）诱导的CREB磷酸化。而在VPAC1/CHO和VPAC2/CHO细胞中，PACAP（1 nM）同样诱导了CREB磷酸化；然而，PA-8（10 pM至10 nM）并未抑制PACAP（1 nM）诱导的CREB磷酸化[1]。 |
| 体内活性 | PA-8 (100 pmol/5 μL；脊髓内注射；一次；雄性ddY小鼠)处理可抑制PACAP引起的逆反应和机械性痛觉过敏现象[1]。PA-8（3-30 mg/kg，口服）治疗能剂量依赖性地减轻甲醛诱导的疼痛反应第二阶段。PA-8还能抑制脊髓背角同侧c-fos的上调[2]。动物模型：注射PACAP（100 pmol）的雄性ddY小鼠（6周龄）[1]剂量：100 pmol/5 μL给药方式：脊髓内注射；一次结果：抑制了PACAP引起的逆反应和机械性痛觉过敏现象。 |
| 分子量 | 342.35 |
| 分子式 | C17H18N4O4 |
| CAS No. | 878437-15-1 |
| Smiles | COc1cc(ccc1OCC=C)C1CC(=O)Nc2nc(N)[nH]c(=O)c12 |
储存&溶解度
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 22.5 mg/mL (65.7 mM), Sonication and heating to 60℃ are recommended. | ||||||||||||||||||||||||||||||
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请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：
比如您的给药剂量是 10 mg/kg ，每只动物体重 20 g ，给药体积 100 μL ， 
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