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Synephrine hydrochloride

Synephrine hydrochloride

产品编号 T6688   CAS 5985-28-4
别名: 辛弗林盐酸盐, Oxedrine hydrochloride, Synephrine HCl

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。

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Synephrine hydrochloride Chemical Structure
Synephrine hydrochloride, CAS 5985-28-4
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
其他形式的 Synephrine hydrochloride:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: Synephrine hydrochloride (T6688)
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纯度: 100%
纯度: 99.63%
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参考文献
植物来源
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 12 mg/mL (58.9 mM)

Ethanol: 4 mg/mL (19.63 mM)

H2O: 38 mg/mL (186.6 mM)

溶液配制表

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

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TargetMol Library Books参考文献

1. Huang YT, et al. Jpn J Pharmacol, 2001, 85(2), 183-188. 2. Hibino T, et al. J Pharmacol Sci, 2009, 111(1), 73-81. 3. Ma G, et al. Planta Med, 2010, 76(10), 981-1986. 4. Hong NY, et al. Biochem Biophys Res Commun, 2012, 418(4), 720-724. 5. Xu W W, Zheng C C, Huang Y N, et al. Synephrine Hydrochloride Suppresses Esophageal Cancer Tumor Growth and Metastatic Potential through Inhibition of Galectin-3-AKT/ERK Signaling[J]. Journal of agricultural and food chemistry. 2018 Sep 5;66(35):9248-9258.

TargetMol Library Books文献引用

1. Xu W W, Zheng C C, Huang Y N, et al. Synephrine Hydrochloride Suppresses Esophageal Cancer Tumor Growth and Metastatic Potential through Inhibition of Galectin-3-AKT/ERK Signaling. Journal of Agricultural and Food Chemistry. 2018 Sep 5;66(35):9248-9258
L-Homoserine γ-Glu-Phe TFA(7432-24-8 free base) Nε,Nε,Nε-Trimethyllysine chloride L-Aspartic acid Nepsilon-Acetyl-L-lysine Dimethylmalonic acid 3-Methyl-2-oxovaleric acid 5'-Guanylic acid disodium salt

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该产品包含在如下化合物库中:
中药单体化合物库 膜蛋白靶向化合物库 GPCR靶点分子库 神经退行性疾病化合物库 生物碱类天然产物库 抗肥胖化合物库 抗癌天然产物库 神经信号分子库 经典已知活性库 抗阿尔茨海默症化合物库

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Keywords

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

 

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