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Semotiadil recemate fumarate

产品编号 T12880 CAS 123388-25-0

Semotiadil recemate fumarate is the recemate of Semotiadil fumarate. Semotiadil fumarate is a novel antagonist of vasoselective Ca2+ channel.

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Semotiadil recemate fumarate Chemical Structure

Semotiadil recemate fumarate, CAS 123388-25-0

规格	价格/CNY	货期
25 mg	￥ 10,600	6-8周
50 mg	￥ 13,800	6-8周
100 mg	￥ 17,500	6-8周

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生物活性

化学信息

存储 & 溶解度

参考文献

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产品描述	Semotiadil recemate fumarate is the recemate of Semotiadil fumarate. Semotiadil fumarate is a novel antagonist of vasoselective Ca2+ channel.
体外活性	Semotiadil(1 μM) produces an inhibition of 12.4±9.7% and in a concentration of 10 μM an inhibition of 25±11.0%[1]. At a holding potential of -100 mV, Semotiadil (> or =0.1 μM; dissolved in DMSO) inhibits the ICa in a concentration-dependent manner (IC50=2.0 μM). At a holding potential of -80 mV or -60 mV, the concentration-inhibition curve observed in the presence of Semotiadil is shifted to the left compared with that observed at -100 mV; 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 (<1 μM) 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[2].
体内活性	Semotiadil fumarate is a novel antagonist of benzothiazine calcium, 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 (10 mg/kg, p.o.) and Enalapril (5 mg/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. Combined daily dosing of Semotiadil, especially with Enalapril, each at relatively low doses may be able to control hypertension in a continuous manner[3].

分子量	652.71
分子式	C33H36N2O10S
CAS No.	123388-25-0

存储

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

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参考文献

1. Koidl B, et al. A novel benzothiazine Ca 2. Teramoto N. Mechanisms of the inhibitory action of Semotiadil fumarate, a novel Ca antagonist, on the voltage-dependent Ca current in smooth muscle cells of the rabbit portal vein. Jpn J Pharmacol. 1993 Mar;61(3):183-95. 3. Ichikawa M, et al. Antihypertensive effects of a novel calcium antagonist, Semotiadil fumarate (SD-3211), alone and in combination with Enalapril or trichlormethiazide in spontaneously hypertensive rats. Biol Pharm Bull. 1994 Nov;17(11):1513-5.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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