Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Synephrine hydrochloride (Oxedrine hydrochloride) 是一种来自Citrus aurantium 的α-adrenergic 和β-adrenergic 激动剂的生物碱,也是一种拟交感神经化合物,能够用于减肥。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 g | ¥ 199 | 现货 | ||
5 g | ¥ 413 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 215 | 现货 |
产品描述 | Synephrine hydrochloride (Oxedrine hydrochloride) is an agonist that acts on sympathomimetic α-adrenergic receptor (AR). |
体外活性 | Synephrine (0.1-30 μM) displays potent vasoconstrictive effects on isolated rat aorta in a dose dependent manner, which can be significantly inhibited by pretreatment with prazosin, BRL15572, and ketanserin but not by pretreatment with SB216641 and propranolol, indicating that Synephrine exerts the constrictive effects via adrenergic alpha(1)-receptors, serotonergic 5-HT(1D) receptors, and 5-HT(2A) receptors. [2] Although the Ki values of Synephrine, 1R,2S-norephedrine, and β-phenethylamine are same for all three subtypes, only Synephrine is a partial agonist of α1A-AR subtype stably expressed in HEK 293 cells with EC50 of 4 μM, giving a maximal response at 100 μM that is equal to 55.3 % of the L-phenylephrine maximum. Functional studies on the α2A- and α2C-AR subtypes stably expressed in CHO cells indicate that Synephrine may act as an antagonist rather than an agonist of the pre-synaptic α(2A)- and α(2C)-AR subtypes present in nerve terminals, although antagonist activity of synephrine is lower than its partial agonist potency. [3] Synephrine (~100 μM) treatment increases basal glucose consumption up to 50% over the control in a dose-dependent manner, without affecting the viability of L6 skeletal muscle cells. Synephrine significantly stimulates the basal- or insulin-stimulated lactic acid production as well as glucose consumption. Synephrine treatment stimulates the phosphorylation of AMPK but not Akt, and Synephrine-induced glucose consumption and the translocation of Glut4 from the cytoplasm to the plasma membrane are sensitive to the inhibition of AMPK but not to the inhibition of PI3 kinase. [4] |
体内活性 | Administration of Synephrine (1 mg/kg per 12 hours) for 8 days significantly improves the hyperdynamic state in portal hypertensive rats induced by either partial portal vein ligation (PVL) or bile duct ligation (BDL), and significantly reduces the portal venous pressure, portal tributary blood flow and cardiac index in both PVL and BDL rats. [1] |
激酶实验 | In vitro kinase assays [1] : To screen for small molecule inhibitors of ATM kinase activity, an in vitro kinase assay is adapted, and an ELISA assay develops which measured the phosphorylation status of the ATM downstream target p53. Recombinant GST-p53(1-101) and full-length Flag-tagged ATM & ATR are purified for use in the ELISA and in vitro kinase assays. Briefly, Nunc 96 well Maxisorp plates are coated overnight (4 °C) with 2μg of purified, recombinant GST-p53(1-101) in PBS. All subsequent incubations are performed at room temperature. The plates are washed (0.05%v/v-Tween/PBS) before addition of purified recombinant full-length ATM kinase (30 ng–60 ng) in a final volume of 80μL of reaction buffer (20 mM HEPES, 50 mM NaCl, 10 mM MgCl2, 10 mM MnCl2, 1 mM DTT and 1 μM ATP) in the presence or absence of CP-466722. CP-466722 (10 μM) is added to plates in duplicate and the kinase assay is incubated (90 minutes). Plates are washed (0.05%v/v-Tween/PBS), blocked (1hour, 1%w/v-BSA/PBS) and rinsed before anti-Phospho(Ser15)-p53 antibody (1:1000/PBS) is added to the plates and incubated (1hour). To reduce non-specific binding plates are washed (0.05%v/v-Tween/PBS) prior to incubation (1hour) with HRP-conjugated goat anti-rabbit IgG secondary antibody (1:5000/PBS). Secondary antibody that is linked to the phosphorylated GST-p53(1–101) protein is detected with TMB substrate reagent. Plates are developed (15 minutes–30 minutes) and the reaction is stopped (1 M H2SO4 final concentration) before absorbance is determined (λ450 nM). CP-466722 that inhibits ATM kinase activity in ELISA assays, are characterized with respect to inhibition of ATM/ATR kinases using in vitro kinase assays. Western blotting using the anti-Phospho(Ser15)-p53 antibody is used as a readout of ATM/ATR inhibition. Extended analysis of CP466722 (10 μM) against a commercially available panel of kinases is performed by Upstate. |
别名 | 辛弗林盐酸盐, Oxedrine hydrochloride, Synephrine HCl |
分子量 | 203.666 |
分子式 | C9H14ClNO2 |
CAS No. | 5985-28-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 12 mg/mL (58.9 mM)
Ethanol: 4 mg/mL (19.63 mM)
H2O: 38 mg/mL (186.6 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol / H2O | 1 mM | 4.91 mL | 24.55 mL | 49.1 mL | 122.75 mL |
5 mM | 0.982 mL | 4.91 mL | 9.82 mL | 24.55 mL | |
10 mM | 0.491 mL | 2.455 mL | 4.91 mL | 12.275 mL | |
DMSO / H2O | 20 mM | 0.2455 mL | 1.2275 mL | 2.455 mL | 6.1375 mL |
50 mM | 0.0982 mL | 0.491 mL | 0.982 mL | 2.455 mL | |
H2O | 100 mM | 0.0491 mL | 0.2455 mL | 0.491 mL | 1.2275 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Synephrine hydrochloride 5985-28-4 GPCR/G Protein Metabolism Neuroscience Endogenous Metabolite Adrenergic Receptor β-adrenergic inhibit Synephrine Inhibitor alkaloid loss α-adrenergic 辛弗林盐酸盐 Oxedrine hydrochloride Beta Receptor Synephrine Hydrochloride Synephrine HCl sympathomimetic weight Oxedrine Oxedrine Hydrochloride inhibitor