辛弗林盐酸盐|T6688|TargetMol

Synephrine hydrochloride
5985-28-4

￥199 1g 起订

上海更新日期：2025-03-12

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产品详情:

中文名称：: 辛弗林盐酸盐

英文名称：: Synephrine hydrochloride

CAS号：: 5985-28-4

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.36%

产品类别：: 抑制剂

货号：: T6688

Product Introduction

Bioactivity

名称	Synephrine hydrochloride
描述	Synephrine hydrochloride (Oxedrine hydrochloride) is an agonist that acts on sympathomimetic α-adrenergic receptor (AR).
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.
体外活性	Synephrine（0.1-30 μM）在剂量依赖的方式下，对分离的大鼠主动脉显示出强烈的血管收缩效应，该效应可被prazosin、BRL15572和ketanserin显著抑制，而SB216641和propranolol的预处理则不能抑制，表明Synephrine通过肾上腺素能α(1)-受体、5-HT(1D)受体和5-HT(2A)受体施加收缩效应。[2] 尽管Synephrine、1R,2S-去甲肾上腺素和β-苯乙胺对所有三个亚型的Ki值相同，但只有Synephrine是在HEK 293细胞中稳定表达的α1A-AR亚型的部分激动剂，其EC50为4 μM，在100 μM时给出的最大反应等于L-苯肾上腺素最大反应的55.3%。在CHO细胞中稳定表达的α2A-和α2C-AR亚型的功能研究表明，尽管Synephrine的拮抗剂活性低于其部分激动剂效力，但Synephrine可能作为神经末梢存在的α(2A)-和α(2C)-AR亚型的拮抗剂而非激动剂。[3] Synephrine（~100 μM）处理以剂量依赖的方式将L6骨骼肌细胞的基础葡萄糖消耗量提高了50%，而不影响细胞的存活性。Synephrine显著刺激基础或胰岛素刺激的乳酸产生以及葡萄糖消耗。Synephrine处理刺激AMPK的磷酸化，但不刺激Akt，并且Synephrine诱导的葡萄糖消耗和Glut4从细胞质到质膜的转移对AMPK的抑制敏感，而不对PI3激酶的抑制敏感。[4]
体内活性	给予Synephrine（1 mg/kg，每12小时一次）连续8天，显著改善了因部分门静脉结扎（PVL）或胆管结扎（BDL）引起的门脉高压大鼠的高动力状态，并且在PVL和BDL大鼠中显著降低了门静脉压力、门静脉分支血流量和心脏指数。[1]
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 16.67 mg/mL (81.83 mM) Ethanol : 4 mg/mL (19.63 mM) H2O : 38 mg/mL (186.6 mM)
关键字	β-adrenergic \| inhibit \| Synephrine \| Inhibitor \| Adrenergic Receptor \| alkaloid \| loss \| α-adrenergic \| Synephrine hydrochloride \| Beta Receptor \| Synephrine Hydrochloride \| Endogenous Metabolite \| sympathomimetic \| weight \| Oxedrine \| Oxedrine Hydrochloride
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辛弗林盐酸盐|||Synephrine HCl|||Oxedrine hydrochloride|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

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