ZM241385

製品コードS8105 バッチS810502

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C16H15N7O2
分子量 337.34 CAS No. 139180-30-6
Solubility (25°C)* 体外 DMSO 67 mg/mL (198.61 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 ZM-241385 is a high affinity antagonist ligand selective for the adenosine A2A receptor.
in vitro ZM 241385 has high affinity for A2a receptors. In rat phaeochromocytoma cell membranes, ZM 241385 displaces binding of tritiated 5'-N-ethylcarboxamidoadenosine (NECA) with a pIC50 of 9.52[3]. ZM241385 delays the appearance of anoxic depolarization (AD), a phenomenon strictly related to cell damage and death, protect from the synaptic activity depression brought about by a severe (7 min) OGD period, and protect CA1 neuron and astrocyte from injury[4].
in vivo ZM-241385 significantly blunts the hypotensive effects of CCPA and NECA without altering the bradycardia induced by these agonists. It blocks the infarct size-reducing effects(cardioprotective effects) of this two distinct adenosine receptor agonists[1].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 PC12 cells
濃度 1 μM
反応時間 24 h
実験の流れ

Nitric oxide (NO) production is assessed by measuring the amount of nitrite, a stable metabolic product of NO that provides an indirect measurement of NO, by using the Griess diazotization reaction. Briefly, 24 h after incubation with 1.0 µM CG21680 or 1.0 µM ZM241385 or exposure to SMF, samples of medium (150 µl) are collected from cells and mixed with 130 µl dH2O and with 20 µl Griess reagent using instruction supplied by the manufacturer. After a 30 min incubation period at room temperature, the samples are evaluated spectrophotometrically at 548 nm and OD values-in comparison with a standard curve is determined in culture medium by using serial dilutions of sodium nitrite-represented total stable metabolites of NO.
動物実験 動物モデル Adult Sprague-Dawley rats 
投薬量 1.5 mg/kg
投与方法 i.v.

カスタマーフィードバック

Data from [Data independently produced by , , Biochem Pharmacol, 2018, doi: 10.1016/j.bcp.2018.01.033]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Adenosine Kinase Inhibition Prevents Severe Acute Pancreatitis via Suppressing Inflammation and Acinar Cell Necroptosis [ Front Cell Dev Biol, 2022, 10:827714] PubMed: 35281076
Exogenous adenosine activates A2A adenosine receptor to inhibit RANKL-induced osteoclastogenesis via AP-1 pathway to facilitate bone repair [ Mol Biol Rep, 2021, 10.1007/s11033-021-07017-1] PubMed: 34846650
Ticagrelor Inhibits the NLRP3 Inflammasome to Protect Against Inflammatory Disease Independent of the P2Y 12 Signaling Pathway [ Cell Mol Immunol, 2020, 10] PubMed: 32523112
Blockade of Adenosine A 2A Receptor Protects Photoreceptors after Retinal Detachment by Inhibiting Inflammation and Oxidative Stress [ Oxid Med Cell Longev, 2020, 2020:7649080] PubMed: 32714489
The Adenosine A2A Receptor Agonist Accelerates Bone Healing and Adjusts Treg/Th17 Cell Balance Through Interleukin 6 [ Biomed Res Int, 2020, 2020:2603873] PubMed: 32382539
The cAMP-Adenosine Feedback Loop Maintains the Suppressive Function of Regulatory T Cells [ J Immunol, 2019, 203(6):1436-1446] PubMed: 31420466
A novel combination of astilbin and low-dose methotrexate respectively targeting A2AAR and its ligand adenosine for the treatment of collagen-induced arthritis [Ma Y Biochem Pharmacol, 2018, 153:269-281] PubMed: 29410374

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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