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化学情報
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Synonyms | ICI-118,551 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
| 化学式 | C17H27NO2.HCl |
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| 分子量 | 313.86 | CAS No. | 72795-01-8 | |
| Solubility (25°C)* | 体外 | DMSO | 62 mg/mL (197.54 mM) | |
| Ethanol | 62 mg/mL (197.54 mM) | |||
| Water | 21 mg/mL (66.9 mM) | |||
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* <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. |
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溶剤液（一定の濃度）を調合する
生物活性
| 製品説明 | Zenidolol (ICI-118551) Hydrochloride is a highly selective β2-adrenergic receptor antagonist with Ki values of 0.7, 49.5 and 611 nM for β2, β1 and β3 receptors, respectively. |
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| in vitro | ICI-118551 inhibits cAMP accumulation by 50% (IC50 = 1.7 mM)[1]. Pharmacological experiments proves that the right shift of the norepinephrine dose-response curve by ICI 118551 is mediated via a beta(2)-adrenoceptor/G(i/o) protein-dependent pathway enhancing NO production in the endothelium; these results are corroborated in beta-adrenoceptor and endothelial NO synthase knockout mice where ICI 118551 has no effect. ICI 118551 increases vascular lumen diameter in lung sections and reduces pulmonary arterial pressure under normoxia and under hypoxia in the isolated perfused lung model[2]. Transgenic mice with high beta(2)AR number and increased G(i) levels have normal basal contractility but show a similar negative inotropic response to ICI 118,551. Overexpression of human beta(2)AR in rabbit myocytes using adenovirus potentiates the negative inotropic effect of ICI 118,551. In human, rabbit, and mouse myocytes, the negative inotropic effects are blocked after treatment of cells with pertussis toxin to inactivate G(i), and overexpression of G(i)alpha(2) induces the effect de novo in normal rat myocytes[5]. |
| in vivo | After 1 week of treatment, ICI 118,551 has no effect on the beta 1-receptor mediated shortening of electromechanical systole (QS2I), the rise in systolic pressure and rise in renin, whereas these responses are blocked by a dose factor of eight after propranolol. ICI 118,551 and propranolol equally block the beta 2-receptor mediated fall in diastolic pressure and the rise in noradrenaline. beta 2-selective blockade by ICI 118,551 lowers blood pressure[4]. |
プロトコル(参考用のみ)
| 細胞アッセイ | 細胞株 | MEF cell line |
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| 濃度 | 10μM | |
| 反応時間 | 2-hours incubation at room-temperature | |
| 実験の流れ | Binding reactions are carried out by incubating 60 μg of membranes with 10 nM [3H]dihydroalprenolol hydrochloride and different concentrations of ICI 118,551. After a two hour incubation at room-temperature, the binding reactions are terminated by rapid filtration over glass fiber filters. Radioactivity in the filters is then quantified using a liquid scintillation counter. Non-specific binding is determined in the presence of 1 μM alprenolol. Binding data are analyzed with GraphPad Prism software. |
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| 動物実験 | 動物モデル | 8-9 weeks old male mice |
| 投薬量 | 1 or 2 mg/kg | |
| 投与方法 | i.p. |
参考
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：
| Testicular Macrophages Produce Progesterone De Novo Promoted by cAMP and Inhibited by M1 Polarization Inducers [ Biomedicines, 2022, 10(2)487] | PubMed: 35203696 |
| Functional solubilization of the β2-adrenoceptor using diisobutylene maleic acid [ iScience, 2021, 24(12):103362] | PubMed: 34825145 |
| Development of 3D-QSAR models for predicting the activities of chemicals to stimulate muscle growth via β2-adrenoceptor [ Toxicol In Vitro, 2021, 77:105251] | PubMed: 34601065 |
| Reactivation of dormant tumor cells by modified lipids derived from stress-activated neutrophils [ Sci Transl Med, 2020, 12(572)eabb5817] | PubMed: 33268511 |
| Acute Stress Induces Visceral Hypersensitivity via Glucocorticoid Receptor-Mediated Membrane Insertion of TRPM8: Involvement of a Non-Receptor Tyrosine Kinase Pyk2 [ Neurogastroenterol Motil, 2020, 11;e13877] | PubMed: 32391653 |
| Local Sympathetic Innervations Modulate the Lung Innate Immune Responses [ Sci Adv, 2020, 13;6(20):eaay1497] | PubMed: 32426489 |
| Depression promotes prostate cancer invasion and metastasis via a sympathetic-cAMP-FAK signaling pathway. [ Oncogene, 2018, 37(22):2953-2966] | PubMed: 29515233 |
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。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。