| 中文名称: | Semotiadil recemate fumarate | ||||
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| 英文名称: | Semotiadil recemate fumarate | ||||
| 别名: | (2R)-2-[2-[3-[2-(1,3-Benzodioxol-5-yloxy)ethyl-methylamino]propoxy]-5-methoxyphenyl]-4-methyl-1,4-benzothiazin-3-one,(E)-but-2-enedioic acid | ||||
| CAS No: | 123388-25-0 | 分子式: | C33H36N2O10S | 分子量: | 652.71 |
| CAS No: | 123388-25-0 | ||||
| 分子式: | C33H36N2O10S | ||||
| 分子量: | 652.71 | ||||
基本信息
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产品编号： |
S11169 |
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产品名称： |
Semotiadil recemate fumarate |
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CAS: |
123388-25-0 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
二年 |
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分子量： |
652.71 |
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化学名： |
(2R)-2-[2-[3-[2-(1,3-Benzodioxol-5-yloxy)ethyl-methylamino]propoxy]-5-methoxyphenyl]-4-methyl-1,4-benzothiazin-3-one,(E)-but-2-enedioic acid |
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Solubility (25°C)： |
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体外:
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DMSO |
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Ethanol |
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Water |
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体内(现配现用): |
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＜1mg/ml表示微溶或不溶。 |
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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。 |
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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。 |
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生物活性
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产品描述 |
Semotiadil fumarate的外消旋体。Semotiadil fumarate是一种新型的血管选择性的Ca2+通道拮抗剂。 |
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靶点 |
Ca2+channel |
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体外研究 |
Semotiadil in a concentration of 1μM produces an inhibition of 12.4±9.7% and in a concentration of 10μM an inhibition of 25±11.0%.Effects of Semotiadil on the voltage-dependent Ca current (ICa) are investigated in dispersed smooth muscle cells of the rabbit portal vein.At a holding potential of-100mV,Semotiadil (>or=0.1μM;dissolved in DMSO) inhibits the ICa in a concentration-dependent manner (IC50=2.0μM).At a holding potential of -80mV or -60 mV,the concentration-inhibition curve observed in the presence of Semotiadil is shifted to the left compared with that observed at -100mV;and Semotiadil shifts the voltage-dependent inactivation curve to the left.The curve for the decay of ICa is fitted with two time constants.Semotiadil (<1μM) reduces the slow but not the fast time constant.The curve for the recovery from ICa inactivation also consisted of two time constants,and Semotiadil (1 microM) prolongs the slow recovery.Semotiadil dissolved in deionized water more potently inhibits ICa than Semotiadil dissolved in DMSO. |
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体内研究 |
Semotiadil fumarate,a novel benzothiazine calcium antagonist,is given alone or in combination with either Enalapril or trichlormethiazide to conscious,spontaneously hypertensive,rats daily for 2 weeks.When given alone,the antihypertensive effects of Semotiadil (10mg/kg,p.o.) and Enalapril (5mg/kg,p.o.) first became apparent after the 3rd dose and thereafter the effects appeared to develop daily although this effect had waned by the time of the next dose.These results indicate that combined daily dosing of Semotiadil,especially with Enalapril,each at relatively low doses may be able to control hypertension in a continuous manner. |
推荐实验方法(仅供参考)
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激酶实验： |
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Semotiadil is dissolved in DMSO.Appropriate dilutions are made freshly for each experiment.The experiments are performed in an experimental bathing chamber (volume 1ml) mounted on the stage of an inverted microscope.The cells are superfused with warm (37℃) extracellular solution at the rate of 3mL/min.The solution could be exchanged for an identical solution containing the substance under study without any significant alteration either in the flow rate or in the temperature of the superfusing fluid.A complete exchange of the bath solution was achieved within 1 min. |
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动物实验: |
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Rats Semotiadil fumarate is given alone or in combination with either Enalapril or trichlormethiazide to conscious,spontaneously hypertensive,rats daily for 2 weeks.Systolic blood pressure and heart rate are recorded 24h before the start of the regimen and then every 2 and 24h after the 1st,3rd,7th,10th and 14th doses.When given alone,the antihypertensive effects of Semotiadil (10mg/kg,p.o.) and Enalapril (5mg/kg,p.o.) first became apparent after the 3rd dose and thereafter the effects appeared to develop daily although this effect had waned by the time of the next dose. |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
