PA-8|cas:878437-15-1|西域试剂

PA-8,97.02%

产品编号：Bellancom-133529| CAS NO：878437-15-1| 分子式：C₁₇H₁₈N₄O₄| 分子量：342.35

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货号	价格	库存与货期
Bellancom-133529	￥1200.00	杭州北京（现货）
Bellancom-133529	￥1800.00	杭州北京（现货）
Bellancom-133529	￥4000.00	杭州北京（现货）
Bellancom-133529	￥7500.00	杭州北京（现货）
Bellancom-133529	￥12800.00	杭州北京（现货）

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PA-8

产品介绍

PA-8 是一种有效的，选择性的，具有口服活性的 PACAP I 型 (PAC1) 受体拮抗剂。PA-8 抑制 PAC1受体中 PACAP 诱导的 CREB 的磷酸化，但不抑制 VPAC1 或 VPAC2 受体。PA-8 还抑制 PACAP 诱导的 cAMP 升高，IC₅₀ 为 2 nM。

生物活性

PA-8 is a potent, selective and orally active PACAP type I (PAC1) receptor antagonist. PA-8 inhibits the phosphorylation of CREB induced by PACAP in PAC1-, but not VPAC1- or VPAC2-receptor. PA-8 also inhibits PACAP-induced cAMP elevation with an IC₅₀ of 2 nM.

体外研究

In PAC1/CHO cells, PA-8 (10 pM to 10 nM; 30 minutes) dose dependently inhibits PACAP (1 nM)-induced CREB phosphorylation. In VPAC1/CHO and VPAC2/CHO cells, PACAP (1 nM) also induced CREB phosphorylation; however, PA-8 (10 pM to 10 nM) does not inhibit PACAP (1 nM)-induced CREB phosphorylation.

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

体内研究

PA-8 (100 pmol/5 µL; intrathecal injection; once; male ddY mice) treatment inhibits PACAP-induced aversive responses and mechanical allodynia in vivo.
PA-8 (3-30 mg/kg, p.o.) treatment results in the dose-dependent attenuation of the second phase of formalin-induced nociceptive responses. PA-8 also inhibits c-fos upregulation in the ipsilateral dorsal horn of the spinal cord.

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

Animal Model:	Male ddY mice (6 weeks old) injected with PACAP (100 pmol)
Dosage:	100 pmol/5 µL
Administration:	Intrathecal injection; once
Result:	Inhibited PACAP-induced aversive responses and mechanical allodynia in vivo.

体内研究

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

Animal Model:	Male ddY mice (6 weeks old) injected with PACAP (100 pmol)
Dosage:	100 pmol/5 µL
Administration:	Intrathecal injection; once
Result:	Inhibited PACAP-induced aversive responses and mechanical allodynia in vivo.

性状

Solid

溶解性数据

In Vitro:

DMSO : 25 mg/mL (73.02 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.9210 mL	14.6049 mL	29.2099 mL
5 mM	0.5842 mL	2.9210 mL	5.8420 mL
10 mM	0.2921 mL	1.4605 mL	2.9210 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: ≥ 2.5 mg/mL (7.30 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.30 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