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Tecadenoson  ≥98%

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包装规格：1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO（≥155 mg/mL）
产品描述：基本信息 产品编号： T10822 产品名称： Tecadenoson CAS: 204512-90-3   储存条件 粉末 -20℃ 四年     分子式： C14H19N5O5 溶于液体 -80℃ 6个月 分子量 337.33 -20℃ 1个月 化学名：  (2R,3S,4R,5R)-2-(hydroxymethyl)-5-[6-[[(3R)-oxolan-3-yl]amino]purin-9-yl]oxolane-3,4-diol Solubility (25°C)：   体外:   DMSO   Ethanol   Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.9645mL 14.8223mL 29.6446mL 5mM 0.5929mL 2.9645mL 5.9289mL 10mM 0.2964mL 1.4822mL 2.9645mL   生物活性 产品描述 一种选择性的腺苷受体 (A1 adenosine receptor) 激动剂。 靶点 Target:A1 adenosine receptor   体外研究 In the atrial-paced isolated heart,Tecadenoson is approximately 5 fold more potent to prolong the stimulus-to-His bundle (S-H interval),a measure of slowing AV nodal conduction (EC50=41nM) than to increase coronary conductance (EC50=200nM).At concentrations of Tecadenoson (40nM) and diltiazem (1μM) that causes equal prolongation of S-H interval (-10ms),diltiazem, but not Tecadenoson,significantly reduces left ventricular developed pressure (LVP) and markedly increases coronary conductance.Tecadenoson shortens atrial (EC50=73nM) but not the ventricular monophasic action potentials (MAP). 体内研究 In atrial-paced anaesthetized guinea-pigs,intravenous infusions of Tecadenoson and diltiazem causes nearly equal prolongations of P-R interval.Tecadenoson (2,5,20μg/kg i.p.) causes a rapid and sustained dose-dependent decrease in NEFA at doses that do not cause bradycardia.Tecadenoson given at 50μg/kg causes a significant bradycardia (50% decrease in heart rate at 25 min.   推荐实验方法(仅供参考) 激酶实验： The effect of Tecadenoson on binding to A1 and A2A-adenosine receptors of porcine forebrain and striatum membranes,respectively,are determined. Assays for A1 and A2A receptors are carried out by using the A1 receptor antagonist [3H]CPX and the A2A receptor agonist [3H]CGS 21680.Membranes are treated with adenosine deaminase (2 U/mL) for 20 min at room temperature prior to and during radioligand binding assays.Membranes (0.2-0.7mg),adenosine deaminase,and the indicated radioligand are incubated for 3h in a 300μL volume of Tris-HCl buffer (50mM) (pH 7.4).Assays are carried out in triplicate at room temperature.After the incubation period,bound and free radioligand are diluted by the addition of icecold Tris-HCl buffer (5mL),and immediately separated by vacuum filtration of assay contents onto Whatman GF/C filters and ishing of trapped membranes with Tris-HCl buffer (20mL).Filter disks containing membrane-bound radioactivity are placed in 4mL Scintiverse, and the radioactivity is quantified by a liquid scintillation counter.Specific binding of [3H]CPX and [3H]CGS 21680 is defined as membrane binding displaced in the presence of CPT (10μM) and R-PIA (10μM),respectively.   动物实验:   Rat:The effects of Tecadenoson on heart rate and to reduce serum NEFA concentration are determined in separate groups of rats to avoid the effects of animal handling and blood sampling on heart rate.Three days before an experiment, a catheter (0.025-mm outer diameter) is implanted in the left common carotid artery of each rat using aseptic conditions and sterile technique.The catheter is tunneled subcutaneously to the dorsal surface.After recovery from anesthesia,rats are placed in metabolic cages to facilitate handling and blood sampling. Blood samples (0.2mL) are drawn before and at various time points after i.p.injection of either Tecadenoson or vehicle (DMSO in saline).A 0.4-mL volume of 1% sodium citrate in saline is administered after withdrawal of each blood sample to replace blood volume and prevent clotting in the carotid artery catheter.Serum is collected from each sample after centrifugation of the clotted blood.Serum samples are stored at −80℃ until analysis.Serum NEFA concentration is determined using an enzymatic colorimetric assay kit.
保存条件：-20℃

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