1、Product Data SheetPhenoxybenzamine hydrochlorideCat. No.: HY-B0431ACAS No.: 63-92-3分式: CHClNO分量: 340.29作靶點: Adrenergic Receptor作通路: GPCR/G Protein; Neuronal Signaling儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數據體外實驗 DMSO : 100 mg/mL (293.87 mM; Need ultrasonic)H2O : 0.1

2、 mg/mL (insoluble)SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 2.9387 mL 14.6933 mL 29.3867 mL5 mM 0.5877 mL 2.9387 mL 5.8773 mL10 mM 0.2939 mL 1.4693 mL 2.9387 mL請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲存時，請在 6 個內使，-20C 儲存時，請在 1 個內使。體內

3、實驗請根據您的實驗動物和給藥式選擇適當的溶解案。以下溶解案都請先按照 In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結果的可靠性，澄 的儲備液可以根據儲存條件，適當保存；體內實驗的作液，建議您現現配，當天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現沉淀、析出現象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.35 mM); Clear solution此案可獲得 2.5 mg/mL (7.35 m

4、M，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.35 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.5 mg/mL (7.35 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取

5、100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (7.35 mM); Clear solution此案可獲得 2.5 mg/mL (7.35 mM，飽和度未知) 的澄 溶液，此案不適于實驗周 期在半個以上的實驗。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Phenoxybenzamine h

6、ydrochloride藥。具有選擇的 -adrenoceptor 和 calmodulin 的抑制劑， 種常的抗壓體外研究 The IC50 (100 nM) derived from the blockade of 3Hyohimbine binding by Phenoxybenzamine hydrochloride issignificantly less than the IC50 (550 nM) for the corresponding reversal by Phenoxybenzamine hydrochloride of theeffects of norepineph

7、rine on cyclic AMP accumulation1. Phenoxybenzamine hydrochloride (50 nM) in conbinationwith Phenoxybenzamine hydrochloridetolamine (1000 nM) enhances Phenoxybenzamine hydrochlorideylephrine-induced contraction compared with pretreatment with Phenoxybenzamine hydrochloride (50 nM) alone inendothelium

8、-intact aortae. Combined treatment with either dexmedetomidine (300 or 1000 nM) andPhenoxybenzamine hydrochloride (50 nM) or Phenoxybenzamine hydrochloridetolamine (1000 nM) andPhenoxybenzamine hydrochloride (50 nM) enhance Phenoxybenzamine hydrochlorideylephrine-induced contractioncompared with Phe

9、noxybenzamine hydrochloride alone (50 nM). In addition, combined treatment withPhenoxybenzamine hydrochloridetolamine and Phenoxybenzamine hydrochloride enhances Phenoxybenzaminehydrochlorideylephrine-induced contraction compared with dexmedetomidine (1000 nM) and Phenoxybenzaminehydrochloride combi

10、ned treatment. Combined treatment with high concentrations of dexmedetomidine (1000 nM)and Phenoxybenzamine hydrochloride enhances Phenoxybenzamine hydrochlorideylephrine-induced contractioncompared with combined treatment with low concentrations of dexmedetomidine (300 nM) and Phenoxybenzaminehydro

11、chloride2. Phenoxybenzamine hydrochloride (0.1-100 M) inhibits glioma proliferation, migration, and invasionand suppresses the tumorigenesis capacity. Phenoxybenzamine hydrochloride also inhibits self-renewal of gliomastem-like cells. Phenoxybenzamine hydrochloride activates LINGO-1 and inhibits the

12、 TrkB-Akt pathway3.Phenoxybenzamine hydrochloride (0.1 M-1 mM) preserves primary neurons within the CA1, CA3 and dentate gyrusand produces a robust neuroprotective effect, and prevents neuronal death from OGD in all regions of thehippocampus when delivered at 2, 4, and 8 h post-OGD at 100 M4.體內研究 Ph

13、enoxybenzamine hydrochloride (20 nM, s.c.) effectively suppresses the tumorigenesis of glioma cells in mice andthe cell density in Phenoxybenzamine hydrochloride-U87MG xenografts decreases significantly3. Phenoxybenzaminehydrochloride (1 mg/kg, i.v.) treated rats shows significant improvements in NS

14、S and foot fault scoring4.PROTOCOLCell Assay 3 After cytometry, 13 cells are implanted in a 96-well plate in 100 L DMEM supplemented with 10 % FBS. Tenmicroliter (10 % of the total volume) WST-1 (Water Soluble Tetrazolium) is added to cells and incubated at 37C for30 min before colorimetric assay wi

15、th 450 nm excitation and 630 nm emission at 24 h intervals up to 96 h. The meanfluorescence value is counted, and the cell number is determined using the standard curve.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal U87MG cells are injected into

16、 both flanks of the nude mice subcutaneously at a dose of 2.03/200 L per side. EightPage 2 of 3 www.MedChemEAdministration 3 days after injection, neoplasm growth is observed macroscopically on both sides of the mice. Then, 20 nMphenoxybenzamine hydrochloride is injected into the right side subcutan

17、eously at a 2-day interval, and the dissolventDMSO is used as control. The tumor volume (V) is determined by measuring the length (a) and the width (b) andcalculated using the equation: V=(ab)2/2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產品發表的科

18、研獻 Protein Cell. 2019 Mar;10(3):178-195.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Lenox, R.H., et al, Alpha 2-adrenergic receptor-mediated regulation of adenylate cyclase in the intact human platelet. Evidence for a receptor reserve.Mol Pharmacol, 1985. 27(1): p. 1-9.2. Byon HJ, et al. Dexmedetomidine Inhibits Phenylephrine-induced Contractions via Alpha-1 Adrenocept