AZD 2066
Based on 1 publication(s) in Google Scholar
AZD-2066 is a selective, orally active and blood-brain barrier-permeating mGluR5 antagonist. AZD 2066 activates the BDNF/trkB signaling pathway. AZD 2066 can be used in the research of neuropathic pain, major depressive disorder and gastroesophageal reflux disease.
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。
- 純度: 99.8%
- CAS 番号: 934282-55-0
- 分子式: C19H16ClN5O2
- 分子量:381.82
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 AZD 2066
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生物活性
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mGluR5 |
AZD 2066 (1-10 μM) inhibits Ca2+ response, with IC50s of 27.2, 3.56, 96.2, and 380 nM in mGlu5/HEK cells and striatal, hippocampal, and cortical cultures respectively[4].
AZD 2066 (1-10 μM) inhibits the oscillatory Ca2+ response which induced by bath application of DHPG (HY-12598A), and blocks either DHPG or Quis effects in mGlu5/HEK cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
AZD-2066 (10 µM, perfusion of brain slide) alleviates dihydroxyphenylglycine (DHPG)-facilitated long-term depression (LTD) expression in chronic social defeat stress (CSDS)-treated mice via BDNF/trkB signaling pathway[5].
AZD-2066 (5 mg/kg, i.p., 2 × 12 h) alleviates chronic social defeat stress (CSDS)-induced depressive behaviors in mice[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats (weighing 240-250 g)[2]
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Dosage:0.03, 0.1, 0.3, 1, 3, 10, 30 mg/kg
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Administration:Oral gavage (p.o.)
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Result:Caused full and dose-dependent AZD9272-appropriate responding.
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Animal Model:Depressive model (C57BL/6 mice were subjected to physical defeats that were generated by a CD-1 aggressor for 5 min every day for 10 days)[5]
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Dosage:5 mg/kg
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Administration:Intraperitoneal injection (i.p.), 2 × 12 h
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Result:Increased social interaction ratio.
Reversed time spent in interaction zone.
Increased sucrose preference scores.
化学情報
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CAS 番号 934282-55-0
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性状 Solid
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分子量 381.82
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分子式 C19H16ClN5O2
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Color White to off-white
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SMILES
CN1C(C2=CC=NC=C2)=NN=C1O[C@@H](C3=NOC(C4=CC(Cl)=CC=C4)=C3)C
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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ACS Chem Neurosci
Location and Cell-Type-Specific Bias of Metabotropic Glutamate Receptor, mGlu5, Negative Allosteric Modulators. [Abstract]2019 Nov 20;10(11):4558-4570. PMID: 31609579
溶剤 & 溶解度
DMSO : 2 mg/mL (5.24 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (275 KB)
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SDS (557 KB)
- English - EN (557 KB)
- Français - FR (557 KB)
- Deutsch - DE (557 KB)
- Norwegian - NO (557 KB)
- Español - ES (557 KB)
- Swedish - SV (557 KB)
- Italian - IT (557 KB)
- Korean - KR (557 KB)
- Portuguese - PT (557 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Kågedal M, et al. A positron emission tomography study in healthy volunteers to estimate mGluR5 receptor occupancy of AZD2066-estimating occupancy in the absence of a reference region. Neuroimage. 2013 Nov 15;82:160-9. [Content Brief]
[2]. Swedberg MD, et al. AZD9272 and AZD2066: selective and highly central nervous system penetrant mGluR5 antagonists characterized by their discriminative effects. J Pharmacol Exp Ther. 2014 Aug;350(2):212-22. [Content Brief]
[3]. Antoniu SA. Discontinued drugs for pulmonary, allergy, gastrointestinal, arthritis (2012). Expert Opin Investig Drugs. 2013 Nov;22(11):1453-64. [Content Brief]
[4]. Jong YI, et al. Location and Cell-Type-Specific Bias of Metabotropic Glutamate Receptor, mGlu5, Negative Allosteric Modulators. ACS Chem Neurosci. 2019 Nov 20;10(11):4558-4570. [Content Brief]
[5]. Jiang X, et al. mGluR5 Facilitates Long-Term Synaptic Depression in a Stress-Induced Depressive Mouse Model. Can J Psychiatry. 2020 May;65(5):347-355. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6190 mL | 13.0952 mL | 26.1904 mL | 65.4759 mL |
| 5 mM | 0.5238 mL | 2.6190 mL | 5.2381 mL | 13.0952 mL |
AZD 2066 関連分類
HY-110255 関連分類
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