Guanabenz Acetate

製品コードS4065 バッチS406502

印刷

化学情報

Chemical Structure Synonyms WY-8678 Acetate Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C8H8Cl2N4.C2H4O2
分子量 291.13 CAS No. 23256-50-0
Solubility (25°C)* 体外 DMSO 15 mg/mL (51.52 mM)
Ethanol 15 mg/mL (51.52 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
4%DMSO 30%PEG300 66%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 40 μL of 125 mg/ml clarified DMSO stock solution to 300 μL of PEG 300, mix evenly to clarify it; then continue to add 660 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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 Guanabenz Acetate (WY-8678) is an selective agonist of α2a-adrenergic receptor, α2b-adrenergic receptor and α2c-adrenergic receptor with pEC50 of 8.25, 7.01 and ~5, respectively.
in vitro Guanabenz at a concentration of 30 μM causes a time-dependent loss of nNOS-activity, which is present in cytosol prepared from rat nNOS transfected HEK 293 cells, with a Ki of 1 μM. Guanabenz can induce a concentration-dependent loss of nNOS activity. Within the first 3 h of treatment, 50 μM Guanabenz decreases the accumulation of nitrite and nitrate by approximately 75% in cells. Treatment of HEK 293 cells for 24 h with Guanabenz (100 μM) causes an approximately 35% decrease in the amount of immunodetectable nNOS protein. Guanabenz enhances proteolysis of the protein with the half-life decreasing by one-half from 20 to 10 h. [2] Guanabenz is active against [ PSI+] prion in the yeast-based assay independent of its agonist activity on α2-adrenergic receptors. Guanabenz (10 μM) promote complete PrPSc clearance in mammalian MovS6 cell-based assay. [3]
in vivo Guanabenz injected i.v. in doses of 0.1 mg/kg causes an initial increase in blood pressure followed by a prolonged fall and a decrease in cardiac output, contractile force and heart rate in anesthetized dogs, which requires the presence of sympathetic tone. Guanabenz inhibits pressor responses to various procedures which initiate general sympathetic discharge. Guanabenz also antagonizes responses to sympathetic nerve stimulation. [4] Guanabenz injected at doses of 0.5 mg/kg and above lowers blood pressure and heart rate in unanesthetized hypertensive rats and dogs. [5]

プロトコル(参考用のみ)

キナーゼアッセイ GTPγ[35S] binding assay
Cell pellets are suspended in cold homogenization buffer [5 mM of Tris-HCl, 5 mM of EDTA, 5 mM of EGTA, 0.1 mM of phenylmethysulfonyl fluoride (PMSF), pH 7.5 at 4 ℃] and lysed using a Polytron P10 disrupter (setting 6, 5-sec burst). The membranes are centrifuged at 34,000 g for 15 min at 4 ℃ and the supernatant is removed. This wash procedure is repeated, and aliquots of membranes are resuspended in 50 mM of Tris, 1 mM of EDTA, 5 mM of MgCl2, 0.1 mM of PMSF, pH 7.4, at 4 ℃ and frozen in aliquots at -70 ℃. Membranes are thawed and diluted with buffer (50 mM of Tris, pH 7.4 at 25 ℃, 5 mM of MgCl2, 100 mM of NaCl, 1 mM of EDTA, 1 mM of dithiothreitol, 1 μM of propranolol, 2 μM of GDP). Membrane protein (4 -10mg) is incubated with 0.3 nM [35S]GTPγS and agonist for 60 min at 25℃. Reactions are terminated by vacuum filtration over GF/B filters pre-treated with 0.5% BSA. Filters are washed with ice-cold wash buffer (50 mM of Tris, 5 mM of MgCl2, 100 mM of NaCl, pH 7.5, at 4 ℃), and incorporated radioactivity is determined using liquid scintillation counting.

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：

Androgen Signaling Regulates SARS-CoV-2 Receptor Levels and Is Associated with Severe COVID-19 Symptoms in Men [ Cell Stem Cell, 2020, 27(6):876-889.e12] PubMed: 33232663
Targeting Super-Enhancer-Driven Oncogenic Transcription by CDK7 Inhibition in Anaplastic Thyroid Carcinoma. [ Thyroid, 2019, 29(6):809-823] PubMed: 30924726

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。