A-740003,861393-28-4

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

A-740003

CAS No. : 861393-28-4

MCE 国际站：A-740003

产品活性：A-740003 是一种有效的，选择性的，竞争性的 P2X7 receptor 拮抗剂，抑制大鼠和人的 P2X7 受体，IC₅₀ 值分别为 18 和 40 nM。

研究领域：Membrane Transporter/Ion Channel

作用靶点：P2X Receptor

In Vitro: A 438079 or A 740003 (10 μM) significantly blocks the sustained phase of the BzATP-induced response. A-740003 infusion reduces SE-induced TNF-α expression in dentate granule cells. A-740003 infusions increases SE-induced neuronal death. A-740003 and A-438079 show significantly greater potency in blocking P2X7 receptor activation across all species compared with other antagonists. A-740003 and A-438079 show greater activity at rat and human, as compared with mouse P2X7 receptors. A-740003 potently blocks agonist-evoked IL-1β release with (IC₅₀=156 nM) and pore formation (IC₅₀=92 nM) in differentiated human THP-1 cells.

In Vivo: Systemic administration of A-740003 produces dose-dependent antinociception in a spinal nerve ligation model (ED₅₀=19 mg/kg i.p.) in the rat. A-740003 also attenuates tactile allodynia in two other models of neuropathic pain, chronic constriction injury of the sciatic nerve and vincristine-induced neuropathy. In addition, A-740003 effectively reduces thermal hyperalgesia observed following intraplantar administration of carrageenan or complete Freund's adjuvant (ED₅₀=38-54 mg/kg i.p.). A-740003 is ineffective in attenuating acute thermal nociception in normal rats and does not alter motor performance at analgesic doses.

相关产品：Bioactive Compound Library Plus | Membrane Transporter/Ion Channel Compound Library | Pyroptosis Compound Library | Neurotransmitter Receptor Compound Library | KN-62 | A 438079 hydrochloride | BzATP triethylammonium salt | Gefapixant | A-804598 | Aurintricarboxylic acid | P2X3 antagonist 34 | AZD9056 hydrochloride | BAY-1797 | JNJ-54175446 | AZ10606120 dihydrochloride | A-317491 | JNJ-47965567 | PPADS tetrasodium | AF-353 | Piromelatine | A 839977 | JNJ-55308942 | NF449 octasodium | Oxatomide | PSB-12062 | (E/Z)-Sivopixant | 5-BDBD | Minodronic acid | α,β-Methylene ATP trisodium | GW791343 dihydrochloride | Eliapixant | NF023 hexasodium

热门产品线：重组蛋白 | 化合物库 | 天然产物 | 染料试剂 | PROTAC | 同位素标记物 | 寡核苷酸

Trending products：Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Dye Reagents | PROTAC | Isotope-Labeled Compounds | Oligonucleotides

品牌介绍:
• MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物；
• 10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
• 设有专业的实验中心和严格的质控、验证体系；
• 提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
• 产品的生物活性多经各国客户实验验证；
• Nature, Cell, Science 等多种TOP期刊及制药专利收录了MCE客户的科研成果；
• 专业团队跟踪前沿的制药及生命科学研究进展，为您提供全球前沿的活性化合物；
• 与世界各大制药公司及知名科研机构建立了长期的合作。