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/ P2X受体 / A 438079 HCl

A 438079 HCl {[allProObj[0].p_purity_real_show]}

货号：A152651 同义名： A-438079 (hydrochloride); A 438079 hydrochloride

A 438079 HCl是一种竞争性的P2X7受体拮抗剂，pIC50为6.9，可抑制人重组P2X7细胞系中Ca2+的流入。

HazMat Fee +

There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
A 438079 HCl 化学结构 CAS号：899431-18-6
A 438079 HCl 化学结构
CAS号：899431-18-6
A 438079 HCl 3D分子结构
CAS号：899431-18-6
A 438079 HCl 化学结构 CAS号：899431-18-6
A 438079 HCl 3D分子结构 CAS号：899431-18-6
规格 价格 会员价 库存 数量
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A 438079 HCl 纯度/质量文件 产品仅供科研

货号：A152651 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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A 438079 HCl 生物活性

靶点

  • P2X receptor

    P2X7, pIC50:6.9
描述 ATP is a key neurotransmitter in this process of inducing and maintaining chronic pain. P2X7 is the glial ATP receptor modulating the pathological pain. A 438079 HCl can inhibits P2X7 with an IC50 of 321 nM in 1321N1 cells. In pharmacokinetic rats, treatment of 10 μM/kg showed low mean plasma and brain levels of the drug, suggesting 84% binding rate to plasma protein. In SNL and CCI rats, treatment of 100 and 300 μM/kg significantly improved withdrawal thresholds with the ED50 of 76 and 100μM/kg respectively without affecting rat rotarod performance. Treatment of 80 μM/kg this drug in SNL rats didn't affect the von Frey-related discharges of hmWDR and mWDR but was effective against high intensity stimulation. Such an treatment also attenuated the evoked responses of neurons to thermal stimulation and decreased the level of spontaneous firing. Besides, A 438079 HCl with concentration of 1 μM reduced the P2X7 receptor agonist in non-neuronal DRG cells. IL-1β release was also inhibited by 75.6% at concentration of 3 μM in a dose- dependent manner[1]. The drug also showed effect on seizure in P10 rat model with the dose range from 0.5 to 50 mg/kg in a dose-dependent manner. And seizure damage was also reduced at either 5 or 15 mg/kg as well as reduced TUNEL staining and decreasing score for neuronal damage. The plasma levels declined rapidly to 2.3 μg/mL within 10 min with the initial concentration of 5 mg/kg of A 438079 HCl in the model, which did not affect cell apoptosis at either 5 or 50 mg/kg[2].

A 438079 HCl 细胞研究

细胞系 浓度 检测类型 检测时间 活性说明 数据源
HEK cells Function assay Activity at rat P2X7 receptor expressed in HEK cells assessed as effect on BzATP-induced ethidium uptake, IC50=0.31623 μM 19191585
HEK293 cells Function assay Antagonist activity at human recombinant P2X7 receptor expressed in HEK293 cells assessed as inhibition of benzoylbenzoic ATP-induced calcium production by FLIPR assay, IC50=0.12303 μM 21536435
human 1321N1 cells Function assay Antagonist activity at human P2X7 receptor expressed in human 1321N1 cells assessed as inhibition of calcium flux by FLIPR, IC50=0.12589 μM 16759108
human THP1 cells Function assay Antagonist activity at P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced ethidium uptake, IC50=0.12589 μM 19191585

A 438079 HCl 动物研究

Dose Mice: 80 mg/kg[3], 50 μmol/kg -200 μmol/kg[4] Rats: min = 5 mg/kg[2], max = 30 mg/kg[5]
Administration i.p.

A 438079 HCl 参考文献

[1]McGaraughty S, Chu KL, et al. P2X7-related modulation of pathological nociception in rats. Neuroscience. 2007 Jun 8;146(4):1817-28.

[2]Mesuret G, Engel T, et al. P2X7 receptor inhibition interrupts the progression of seizures in immature rats and reduces hippocampal damage. CNS Neurosci Ther. 2014;20(6):556-64.

[3]Xie Y, Williams CD, et al. Purinergic receptor antagonist A438079 protects against acetaminophen-induced liver injury by inhibiting p450 isoenzymes, not by inflammasome activation. Toxicol Sci. 2013;131(1):325-35.

[4]Martins JP, Silva RB, et al. The role of P2X7 purinergic receptors in inflammatory and nociceptive changes accompanying cyclophosphamide-induced haemorrhagic cystitis in mice. Br J Pharmacol. 2012;165(1):183-96.

[5]Zhao H, Zhang X, et al. P2X7 Receptor Suppression Preserves Blood-Brain Barrier through Inhibiting RhoA Activation after Experimental Intracerebral Hemorrhage in Rats. Sci Rep. 2016.

A 438079 HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.92mL

0.58mL

0.29mL

14.59mL

2.92mL

1.46mL

29.19mL

5.84mL

2.92mL

A 438079 HCl 技术信息

CAS号899431-18-6
分子式C13H10Cl3N5
分子量 342.61
SMILES Code ClC1=C(Cl)C(C2=NN=NN2CC3=CC=CN=C3)=CC=C1.[H]Cl
MDL No. MFCD09971142
别名 A-438079 (hydrochloride); A 438079 hydrochloride
运输蓝冰
InChI Key MBTJFFMIPPMRGR-UHFFFAOYSA-N
Pubchem ID 11688742
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere, 2-8°C
溶解方案

DMSO: 105 mg/mL(306.47 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 1 mg/mL(2.92 mM)，配合低频超声，并水浴加热至45℃助溶

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案一
方案二
动物实验配方

PO 0.5% CMC-Na 40 mg/mL suspension

Tags: A 438079 | 899431-18-6 | A438079 | A-438079 | P2X7 Receptor Antagonist | Membrane Transporter/Ion Channel | P2X Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | A 438079 HCl 纯度/质量文件 | A 438079 HCl 生物活性 | A 438079 HCl 细胞研究 | A 438079 HCl 动物研究 | A 438079 HCl 参考文献 | A 438079 HCl 实验方案 | A 438079 HCl 技术信息

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