Glaucine hydrobromide
Glaucine hydrobromide (O,O-Dimethylisoboldine hydrobromide; S-(+)-Glaucine hydrobromide; NSC 34396 hydrobromide) is an alkaloid extracted from Glaucium flavum that possesses various activities, including cough relief, bronchodilation, anti-inflammatory effects, analgesia, antipyretic properties, and anticancer effects. Glaucine hydrobromide acts as a selective and orally active inhibitor of phosphodiesterase 4 (PDE4), with a Ki of 3.4 µM in human bronchial tissues and polymorphonuclear leukocytes. Glaucine hydrobromide induces relaxation of human isolated bronchi by antagonizing calcium channels. Additionally, Glaucine hydrobromide inhibits the activation of NF-κB, leading to a reduction in the expression of the MMP-9 gene, thereby suppressing the migration and invasion of breast cancer cells. Therefore, Glaucine hydrobromide holds potential for research in asthma and breast cancer.
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- CAS 番号: 5996-06-5
- 分子式: C21H26BrNO4
- 分子量:436.34
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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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生物活性
製品説明
IC50 & Target
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PDE4 |
体外実験
Glaucine (0.1 μM-1 mM; 30 min) hydrobromide produces a concentration-dependent inhibition of both spontaneous tension and histamine (HY-B1204)-induced tension in isolated human bronchial tissues[1]. Glaucine (10 μM-1 mM; 30 min) hydrobromide concentration-dependently inhibits the concentration of calcium ions in isolated human bronchial tissues induced by potassium depolarization[1]. Glaucine (0.1-3 mM; 120 min) hydrobromide concentration-dependently inhibits the release of peroxidase from human eosinophils[1]. Glaucine (0-50 μM; 24 and 48 h) hydrobromide inhibits the proliferation of MCF-7 cells induced by Phorbol 12-myristate 13-acetate (HY-18739) in a concentration-dependent manner[4]. Glaucine (0-30 μM; 36 h) hydrobromide significantly blocks the expression and activity of MMP-9 in MCF-7 cells induced by Phorbol 12-myristate 13-acetate (HY-18739) in a dose-dependent manner[4]. Glaucine (0-30 μM; 24 h) hydrobromide significantly inhibits the invasion of MDA-MB-231 cells in a dose-dependent manner[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PMA-induced MCF-7 cells
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Concentration:0, 1, 3, 15, 30 and 50 µM
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Incubation Time:24 and 48 h
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Result:Inhibited PMA-induced colony formation by 48 and 63 % at a dose of 15 and 30 µM.
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Cell Line:PMA-induced MCF-7 cells
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Concentration:0, 15 and 30 µM
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Incubation Time:36 h
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Result:Inhibited PMA-induced phosphorylation of IκBα in a dose-dependent manner and decreased nuclear NF-κB p65 subunit levels.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Ovalbumins (HY-W250978) sensitized guinea pigs to inhaled aerosol antigens[5]
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Dosage:10 mg/mL
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Administration:inhale; 10 min
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Result:Reduced airway hyperresponsiveness to histamine and lung eosinophil accumulation 30 minutes and 3 hours after inhalation of the antigen. Increased eosinophil peroxidase activity in bronchoalveolar lavage fluid 24 hours after inhalation of aerosol antigen.
化学情報
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CAS 番号 5996-06-5
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分子量 436.34
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分子式 C21H26BrNO4
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SMILES
CN1CCC2=CC(OC)=C(OC)C3=C2[C@]1([H])CC4=CC(OC)=C(OC)C=C34.Br
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別名
O,O-Dimethylisoboldine hydrobromide; S-(+)-Glaucine hydrobromide; NSC 34396 hydrobromide
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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
[1]. J Cortijo, et al. Bronchodilator and Anti-Inflammatory Activities of Glaucine: In Vitro Studies in Human Airway Smooth Muscle and Polymorphonuclear Leukocytes. Br J Pharmacol. 1999 Aug;127(7):1641-51. [Content Brief]
[2]. Golo M J Meyer, et al. Studies on the in Vivo Contribution of Human Cytochrome P450s to the Hepatic Metabolism of Glaucine, a New Drug of Abuse. Biochem Pharmacol. 2013 Nov 15;86(10):1497-506. [Content Brief]
[3]. Maya Spasova, et al. Cinnamoyl- And Hydroxycinnamoyl Amides of Glaucine and Their Antioxidative and Antiviral Activities. Bioorg Med Chem. 2008 Aug 1;16(15):7457-61. [Content Brief]
[4]. Hyereen Kang, et al. "Glaucine inhibits breast cancer cell migration and invasion by inhibiting MMP-9 gene expression through the suppression of NF-κB activation." Molecular and cellular biochemistry 403 (2015): 85-94. [Content Brief]
[5]. Pons, et al. "Effects of inhaled glaucine on pulmonary responses to antigen in sensitized guinea pigs." European journal of pharmacology 397.1 (2000): 187-195. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Glaucine hydrobromide 関連分類
HY-W726101 関連分類
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