A-286501
A-286501 is an orally active adenosine kinase inhibitor with an IC50 of 0.47 nM (rat brain cytosol). A-286501 blocks the phosphorylation of adenosine to AMP and increases adenosine. A-286501 mediates non-opioid adenosine receptor-dependent antinociceptive and anti-inflammatory effects, reduces paw edema, myeloperoxidase activity, and tactile allodynia, and produces antinociceptive effects in acute, inflammatory, neuropathic, and hyperalgesic models. A-286501 can be used in research on inflammatory pain, neuropathic pain, and diabetic neuropathy.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 483341-15-7
- 分子式: C11H14BrN5O2
- 分子量:328.17
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| IMR-32 | IC50 |
11.6 nM
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Inhibition of adenosine kinase (AK) activity in intact cultured human IMR-32 neuroblastoma cells.
Inhibition of adenosine kinase (AK) activity in intact cultured human IMR-32 neuroblastoma cells.
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11932067 |
体外実験
A-286501 (100 nM; 18 h) is a reversible AK inhibitor that exhibits competitive inhibition with respect to Adenosine (ADO) (HY-B0228) (Ki = 1.87 nM) and noncompetitive inhibition with respect to MgATP2− (Ki = 8.86 nM) when using rat brain cytosolic AK and human recombinant AK[1].
A-286501 exhibits much higher selectivity for AK than for ADO receptors, ADO transporters, ADO deaminase, P2 receptors, and a broad 86-target panel, with IC50 values greater than 100 μM at ADO-related sites and IC50 values greater than 10 μM in the Cerep panel[1].
A-286501 inhibits ADO phosphorylation in intact IMR-32 human neuroblastoma cells with an IC50 of 11.6 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 483341-15-7
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分子量 328.17
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分子式 C11H14BrN5O2
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SMILES
O[C@H]1[C@@H](C[C@@H]([C@H]1O)N)N2C3=NC=NC(N)=C3C(Br)=C2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
A-286501 関連分類
HY-116005 関連分類
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