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McN5691  ≥98%

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包装规格：1mg in glass bottle
产品描述：基本信息 产品编号： M11267 产品名称： McN5691 CAS: 99254-95-2   储存条件 粉末 -20℃ 四年 分子式： C30H35NO3 溶于液体 -80℃ 二年 分子量： 457.60     化学名：  N-(2-(3,4-dimethoxyphenyl)-ethyl)-5-methoxy-N,alphadimethyl-2-(phenylethynyl)benzenepropanamine 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。   生物活性 产品描述 一种电压依赖性钙通道(calciumchannel)阻滞剂。 靶点 Calcium Channel   体外研究 McN5691 (1 and 10μM) prevents 60mM KCl-induced contraction and calcium uptake and causes concentration-dependent relaxation (EC50=190μM) of 30mM KCl-contracted aortic rings.At or below 10μM,McN5691 (McN-5691) has no effects on basal tone or calcium uptake (45Ca) in isolated rings of rabbit thoracic aorta.McN5691 causes complete high affinity inhibition (Kd=39.5nM) of specific diltiazem binding to the benzothiazepine receptor on the voltage-sensitive calcium channel in skeletal muscle microsomal membranes.In contrast to diltiazem,McN5691 inhibits specific dihydropyridine receptor binding,but the effect is biphasic with high (Kd=4.7nM) and low (Kd=919.8nM) affinity components.McN5691 inhibits norepinephrine (NE)-induced contraction (10μM) and calcium uptake (1 and 10μM) and causes concentrationdependent relaxation (EC50=159μM) of 1μM NE-contracted rings of rabbit thoracic aorta. 体内研究 The excretion and metabolism of a 2-ethynylbenzenealkanamine analog,antihypertensive McN5691 (RWJ-26240),in beagle dogs is investigated.A total of 96.8% and 2.8% of the radioactive dose are excreted in feces and urine,respectively,during the 7 days after oral administration of 14C-McN5691.Of the radioactive dose,96.8% and 2.8% is recovered in feces and urine,respectively,in the 7 days after oral administration of 14C-McN5691.More than 87% of the dose is excreted in feces during the 48 hours.McN5691 is extensively metabolized in dogs.Unchanged McN5691 is found in less than 0.1% and 19% of the dose in the 0-24 hour urine and 0-48 hour fecal extract,respectively,and 36% of the sample in the 4 hour plasma.In the McN5691 (McN-5691) study,vascular resistances tend to be higher in spontaneously hypertensive rat (SHR) than in WistarKyoto (WKY) but the differences are statistically significant only in the cerebellum and the midbrain.   推荐实验方法(仅供参考) 动物实验:   Dogs 14C-McN5691 is administered by gavage to male and female beagle dogs (3 of each sex,weight 10.2-12.8kg) as a single 6mg/kg (as free base in corn oil) dose.Plasma samples are obtained for 24 hours after dosing.Urine and fecal samples are collected over a 7-day period.Each collected sample is assayed for total radioactivity and analyzed by TLC and HPLC. Rats Studies are conducted in male SHR and control normotensive Wistar-Kyoto (WKY) rats.All animals are housed in constant temperature and environment facilities and given standard lab chow and water ad libitum.Four separate studies are conducted using conscious,age-matched animals:(a) SHR receiving McN5691 as a hydrochloride salt (McN5691) (n=8,body weight=361±7g);(b) SHR receiving vehicle (VH) (n= 8,bodyweight=381±5g);(C) WKY receiving McN5691(n=9,body weight=355±7g);and (d) WKY receiving VH (n=6,body weight=342±7g).McN5691 or VH alone is administered i.v.(right jugular vein) as a 15 min continuous infusion for each dose.Each animal receives three doses of McN5691 (0.3,1.0 and 3.0mg/kg) in a cumulative fashion or VH infused at an equal rate (0.0408mL/min).
保存条件：-20℃

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