A 839977|cas:870061-27-1|西域试剂

A 839977,98.01%

产品编号：Bellancom-13954| CAS NO：870061-27-1| 分子式：C₁₉H₁₄Cl₂N₆O| 分子量：413.26

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	包装	价格	库存与货期	购买量	操作
Bellancom-13954		￥1256.00	杭州北京（现货）
Bellancom-13954		￥5115.00	杭州北京（现货）

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A 839977

产品介绍

A 839977是一种选择性 P2X7 受体拮抗剂, 可阻断人和大小鼠 P2X7 受体的 BzATP 诱发的钙内流 (IC₅₀s=20 nM, 42 nM / 150 nM); 在体实验中, 通过阻断 IL-1β 释放产生抗痛觉过敏反应, 减弱模型动物的炎症反应与神经性疼痛.

生物活性

A 839977 is a P2X7 selective antagonist; it blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC₅₀ values are 20 nM, 42 nM and 150 nM respectively) and reduces inflammatory and neuropathic pain in animal models; the antihyperalgesic effects of P2X7 receptor blockade are mediated by blocking the release of IL-1beta.

体外研究

A 839977 selectively blocks BzATP-evoked calcium influx at mammalian P2X7 receptors, (IC₅₀=20-150 nM), which blocks agonist-evoked YO-PRO uptake and IL-1beta release from differentiated human THP-1 cells, it has been shown to reduce inflammatory and neuropathic pain in animal models.
A 839977 (50 nM, pre-treatment 1 hour) significantly prevents pressure-induced rise of IL-1β priming in optic nerve astrocytes.

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

RT-PCR

Cell Line:	Optic nerve astrocyte cells
Concentration:	50 nM
Incubation Time:	1 hour(pre-treatment)
Result:	Prevented the IL-1β priming in astrocyte cells

体内研究
(In Vivo)

A 839977 (30 μmol/kg, 100 μmol/kg, 300 μmol/kg; pre-injected 30mins) dose-dependently reduces thermal hyperalgesia produced by intraplantar administration of complete Freund's adjuvant (CFA) in rats.
A 839977 (10 μmol/kg, 30 μmol/kg, 100 μmol/kg; pre-injected 30mins) produces robust antihyperalgesia in the CFA model of inflammatory pain in wild-type mice, but it has no effect on IL-1alphabeta knockout mice.
A 839977 attenuates dorsal horn neuronal responses in cancer bearing animals.

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

Animal Model:	Male Sprague-Dawley, BALB/c mice and IL-1^(−/−) mice for CFA-induced chronic inflammatory
Dosage:	30 μmol/kg, 100 μmol/kg, 300 μmol/kg (rat); 10 μmol/kg, 30 μmol/kg, 100 μmol/kg (mice)
Administration:	Injection; pre-injected 30mins
Result:	Attenuated CFA-induced thermal hyperalgesia in a dose-related manner in rat and mice, but has no effect on IL-1^(−/−) mice.

体内研究

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

Animal Model:	Male Sprague-Dawley, BALB/c mice and IL-1^(−/−) mice for CFA-induced chronic inflammatory
Dosage:	30 μmol/kg, 100 μmol/kg, 300 μmol/kg (rat); 10 μmol/kg, 30 μmol/kg, 100 μmol/kg (mice)
Administration:	Injection; pre-injected 30mins
Result:	Attenuated CFA-induced thermal hyperalgesia in a dose-related manner in rat and mice, but has no effect on IL-1^(−/−) mice.

体内研究

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

Animal Model:	Male Sprague-Dawley, BALB/c mice and IL-1^(−/−) mice for CFA-induced chronic inflammatory
Dosage:	30 μmol/kg, 100 μmol/kg, 300 μmol/kg (rat); 10 μmol/kg, 30 μmol/kg, 100 μmol/kg (mice)
Administration:	Injection; pre-injected 30mins
Result:	Attenuated CFA-induced thermal hyperalgesia in a dose-related manner in rat and mice, but has no effect on IL-1^(−/−) mice.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (241.98 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4198 mL	12.0989 mL	24.1978 mL
5 mM	0.4840 mL	2.4198 mL	4.8396 mL
10 mM	0.2420 mL	1.2099 mL	2.4198 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 (6.05 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.05 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 (6.05 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (6.05 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.05 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.05 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
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玉米油中，混合均匀。