A 438079 NEW
| Price | $41 | $66 | $98 |
| Package | 2mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-12 |
Product Details
| Product Name: A 438079 | CAS No.: 899507-36-9 |
| Purity: 99.70% | Supply Ability: 10g |
| Release date: 2024/11/12 |
Product Introduction
Bioactivity
| 名稱 | A 438079 |
| 描述 | A 438079 is a potent and selective antagonist of the P2X7 receptor (pIC50: 6.9). |
| 激酶實驗 | Human astrocytoma cells, 1321N1, are grown to stably express rat P2X7, human P2X4, P2X2a, P2X2/3, P2X1, P2Y1 and P2Y2 recombinant receptors. Agonist, BzATP, 2,3-O-(4-ben-zoylbenzoyl)-ATP or ATP-induced changes in intracellular Ca2+ concentrations are assessed in all of the cell lines using the Ca2+ chelating dye, Fluo-4, in conjunction with a Fluorometric Imaging Plate Reader. The cells are plated out the day before the experiment onto poly-D-lysine-coated black 96 well plates. After the agonist addition, changes in intracellular Ca2+ concentrations are recorded, per second, for 3 min. Ligands are tested at 11 half-log concentrations from 0.1nM to 100 μM. BzATP or ATP concentrations corresponds to the EC70 values for each receptor to enable comparison of antagonist potencies across the multiple P2 receptor subtypes. A 438079 is added to the cell plate and ?uorescence data are collected for 3 min before the addition of agonist, subsequently, data are then collected for another 2 min. The pEC50 or pIC50 values are derived from a single curve ?t [1]. |
| 動物實驗 | To confirm A 438079 reach the brain after systemic administration, P10 rat pups are injected with 5 mg/kg A 438079 and killed either 10 min, 30 min, or 2 h later (n=4 per group). Blood samples are centrifuged at 1000×g for 10 min to isolate the plasma. Samples are analyzed using LC-MS/MS by a service provider. Briefly, protein is precipitated from 50 μL aliquots of the individual plasma or brain tissue homogenate, and A 438079 is quantified by LC-MS/MS from a five-point standard curve [2]. |
| 體外活性 | A 438079 blocks BzATP-(10 μM) evoked changes in intracellular calcium concentrations with an IC50 of 321 nM in 1321N1 cells stably expressing rat P2X7 receptors. A 438079 is also selective for the P2X7 receptor, at concentrations up to 100 μM[1]. |
| 體內(nèi)活性 | In neuropathic rats noxious and innocuous evoked activity of different classes of spinal neurons is reduced by A 438079 (80 μmol/kg, i.v.), and it significantly raises withdrawal thresh-olds in both the SNL and CCI models[1]. A 438079 has superior neuroprotective effects compared with an equal dose of phenobarbital (25 mg/kg)[2]. A 438079 partially but significantly prevents the 6-OHDA-induced depletion of striatal DA stores[3]. Pretreatment with A 438079 reduces nociceptive behavior scores in the HC model[4]. |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 100 mg/mL (326.64 mM), Sonication is recommended. H2O : 0.2 mg/mL (0.65 mM), Sonication is recommended. |
| 關鍵字 | Inhibitor | P2X Receptor | inhibit | A 438079 | P2XRs | A438079 | A-438079 |
| 相關產(chǎn)品 | Opiranserin hydrochloride | Aurintricarboxylic acid | (E/Z)-Sivopixant | PSB-12062 | ATP disodium salt | Oxatomide | JNJ-55308942 | JNJ-42253432 | Ivermectin | Lappaconitine | CTP disodium dihydrate | Brilliant blue G-250 |
| 相關庫 | 經(jīng)典已知活性庫 | 神經(jīng)信號分子庫 | 膜蛋白靶向化合物庫 | 抑制劑庫 | NO PAINS 化合物庫 | 已知活性化合物庫 | 離子通道庫 | 抗癌化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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