Phenoxybenzamine-hydrochloride - Adrenergic Receptor Antagonist - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPhenoxybenzamine 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(shù)據(jù)體外實驗

2、DMSO : 100 mg/mL (293.87 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.35 mM); Clear solution2. 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 solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oil1/3 Master of Small Molecules 您邊的抑制劑師w

3、ww.MedChemESolubility: 2.5 mg/mL (7.35 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Phenoxybenzamine hydrochloride具有選擇的 -adrenoceptor 和 calmodulin 的抑制劑， 種常的抗壓藥。體外研究 The IC50 (100 nM) derived from the blockade of 3Hyohimbine binding by Phenoxybenzamine hydrochlorideis significantly less than the IC50 (5

4、50 nM) for the corresponding reversal by Phenoxybenzaminehydrochloride of the effects of norepinephrine on cyclic AMP accumulation 1. Phenoxybenzaminehydrochloride (50 nM) in conbination with Phenoxybenzamine hydrochloridetolamine (1000 nM) enhancesPhenoxybenzamine hydrochlorideylephrine-induced con

5、traction compared with pretreatment withPhenoxybenzamine hydrochloride (50 nM) alone in endothelium-intact aortae. Combined treatment witheither dexmedetomidine (300 or 1000 nM) and Phenoxybenzamine hydrochloride (50 nM) orPhenoxybenzamine hydrochloridetolamine (1000 nM) and Phenoxybenzamine hydroch

6、loride (50 nM)enhance Phenoxybenzamine hydrochlorideylephrine-induced contraction compared with Phenoxybenzaminehydrochloride alone (50 nM). In addition, combined treatment with Phenoxybenzamine hydrochloridetolamineand Phenoxybenzamine hydrochloride enhances Phenoxybenzamine hydrochlorideylephrine-

7、inducedcontraction compared with dexmedetomidine (1000 nM) and Phenoxybenzamine hydrochloride combinedtreatment. Combined treatment with high concentrations of dexmedetomidine (1000 nM) andPhenoxybenzamine hydrochloride enhances Phenoxybenzamine hydrochlorideylephrine-induced contractioncompared wit

8、h combined treatment with low concentrations of dexmedetomidine (300 nM) andPhenoxybenzamine hydrochloride 2. Phenoxybenzamine hydrochloride (0.1-100 M) inhibits gliomaproliferation, migration, and invasion and suppresses the tumorigenesis capacity. Phenoxybenzaminehydrochloride also inhibits self-r

9、enewal of glioma stem-like cells. Phenoxybenzamine hydrochloride activatesLINGO-1 and inhibits the TrkB-Akt pathway 3. Phenoxybenzamine hydrochloride (0.1 M-1 mM) preservesprimary neurons within the CA1, CA3 and dentate gyrus and produces a robust neuroprotective effect, andprevents neuronal death f

10、rom OGD in all regions of the hippocampus when delivered at 2, 4, and 8 h post-OGD at 100 M 4.體內研究 Phenoxybenzamine hydrochloride (20 nM, s.c.) effectively suppresses the tumorigenesis of glioma cells inmice and the cell density in Phenoxybenzamine hydrochloride-U87MG xenografts decreases significan

11、tly 3.Phenoxybenzamine hydrochloride (1 mg/kg, i.v.) treated rats shows significant improvements in NSS andfoot fault scoring 4.PROTOCOLCell Assay 3 After cytometry, 13 cells are implanted in a 96-well plate in 100 L DMEM supplemented with 10 % FBS.Ten microliter (10 % of the total volume) WST-1 (Wa

12、ter Soluble Tetrazolium) is added to cells and incubatedat 37C for 30 min before colorimetric assay with 450 nm excitation and 630 nm emission at 24 h intervals upto 96 h. The mean fluorescence value is counted, and the cell number is determined using the standardcurve.2/3 Master of Small Molecules

13、您邊的抑制劑師www.MedChemEMCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal U87MG cells are injected into both flanks of the nude mice subcutaneously at a dose of 2.03/200 L perAdministration 3 side. Eight days after injection, neoplasm growth is observed

14、 macroscopically on both sides of the mice.Then, 20 nM phenoxybenzamine hydrochloride is injected into the right side subcutaneously at a 2-dayinterval, and the dissolvent DMSO is used as control. The tumor volume (V) is determined by measuring thelength (a) and the width (b) and calculated using th

15、e equation: V=(ab)2/2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻 Protein Cell. 2019 Mar;10(3):178-195.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Lenox, R.H., et al, Alpha 2-adrenergic receptor-mediated regulat

16、ion of adenylate cyclase in the intact human platelet. Evidence for areceptor reserve. Mol Pharmacol, 1985. 27(1): p. 1-9.2. Byon HJ, et al. Dexmedetomidine Inhibits Phenylephrine-induced Contractions via Alpha-1 Adrenoceptor Blockade and Nitric OxideRelease in Isolated Rat Aortae. Int J Med Sci. 2017 Feb 7;14(2):143-149.3. Lin XB, et al. Anti-tumor activity of phenoxybenzamine hydrochloride on malignant glioma cells. Tumour Biol. 2016 Mar;37(3):2901-8.4. Rau TF, et al. Phenoxybenzamine is neuroprotective in a rat model of severe traumatic b