|3-((5-(2,3-二氯苯基)-1H-四唑-1-基)甲基)吡啶盐酸盐|CsnPharm

CAS No.: 899431-18-6

A 438079 HCl Catalog No. CSN18546

Synonyms: A-438079 (hydrochloride);A-438079 ;A-438079 HCl

A 438079 HCl is a competitive P2X7 receptor antagonist (pIC50 = 6.9 for the inhibition of Ca2+ influx in the human recombinant P2X7 cell line).

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 P2X7 Receptor

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].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

更多
动物研究
剂量
Mice: 80 mg/kg^[3], 50 μmol/kg -200 μmol/kg^[4] Rats: min = 5 mg/kg^[2], max = 30 mg/kg^[5]

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 80 mg/kg^[3], 50 μmol/kg -200 μmol/kg^[4] Rats: min = 5 mg/kg^[2], max = 30 mg/kg^[5]
给药途径	i.p.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.9188 mL
- 14.5939 mL
- 29.1877 mL
- 5 mM
- 0.5838 mL
- 2.9188 mL
- 5.8375 mL
- 10 mM
- 0.2919 mL
- 1.4594 mL
- 2.9188 mL

技术信息

CAS号

899431-18-6

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C13H10Cl3N5

运输

蓝冰

分子量

342.61

别名

A-438079 (hydrochloride);A-438079 ;A-438079 HCl

溶解度

DMSO	165.0 mg/mL (481.6 mM) warming
Water	120.0 mg/mL (350.3 mM)

动物实验配方

0.5% CMC-Na

40 mg/mL

suspension

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

A 438079 HCl Catalog No. CSN18546

靶点选择性

请登录您的专属账户

确认信息