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KT-362 fumarate

产品编号 T27753 CAS 105394-80-7

别名: KT 362, KT362, KT-362

KT-362 fumarate 是一种新型化合物，可作为钙通道、钾通道和钠通道的拮抗剂.KT-362 fumarate 通过影响心房肌肉细胞内钙动员导致血管舒张。KT-362 fumarate 对兔子的股动脉和基底动脉条有放松作用。

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KT-362 fumarate, CAS 105394-80-7

规格	价格/CNY	货期
1 mg	￥ 2,260	现货
5 mg	￥ 5,220	现货
10 mg	￥ 7,380	现货
25 mg	￥ 10,900	现货
50 mg	￥ 14,700	现货
100 mg	￥ 19,900	现货
500 mg	￥ 39,900	现货
1 mL * 10 mM (in DMSO)	￥ 6,130	现货

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其他形式的 KT-362 fumarate:

KT-362 free base
现货

选择批次

纯度: 99.90%

纯度: 99.87%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	KT-362 fumarate is a novel compound that acts as an antagonist of calcium channels, potassium channels and sodium channels.KT-362 fumarate causes vasodilation by affecting intracellular calcium mobilization in atrial muscle cells.KT-362 fumarate has a relaxing effect on femoral and basilar artery strips in rabbits.
体外活性	We studied the effects of KT-362, (5-[3[2-(3,4-dimethoxyphenyl)ethyl]amino]-1-oxopropyl]-2,3,4,5- tetrahydro-1,5-benzothiazepine fumarate), a newly synthesized vasodilating and antiarrhythmic agent, on membrane currents of single guinea pig ventricular cells, using whole-cell voltage-clamp techniques. In the steady state with a stimulation frequency of 0.5 Hz, KT-362 at concentrations of 10 and 30 microM decreased the peak sodium current (INa) in a concentration-dependent manner, i.e., by 27% and 49%, respectively. KT-362 (30 microM) inhibited INa by 21% at 0.2 Hz and by 51% at 1 Hz. In addition, KT-362 (10-30 microM) decreased the L-type Ca current (ICa) in a concentration-dependent fashion. KT-362 (10-300 microM) decreased the maximum rate of rise of action potentials provoked at normal (2.7 mM) K+ concentration and that provoked at high (20 mM) K+ concentration. KT-362 at concentrations over 100 microM significantly depolarized the resting membrane, and the action potential duration remained unaltered. From these findings, we conclude that apart from the alleged inhibitory effects of this agent on the release of calcium from sarcoplasmic reticulum (it is therefore termed 'an intracellular Ca++ blocker'), KT-362 suppresses a variety of membrane ionic currents of cardiac cells.(ABSTRACT TRUNCATED AT 250 WORDS).[1]
体内活性	The effects of a new intracellular calcium antagonist, KT-362 (5-[3-[[2-(3,4-dimethoxyphenyl)-ethyl]amino]-1-oxopropyl]- 2,3,4,5,-tetrahydro-1,5-benzothiazepine fumarate) on myocardial infarct size following a 90-min occlusion and 3-h reperfusion of the left anterior descending coronary artery (LAD) were determined in anesthetized dogs. KT-362 (300 micrograms/kg/min for 20 min followed by 150 micrograms/kg/min for 80 min) was administered intravenously (i.v.) 10 min prior to coronary occlusion and continued throughout the occlusion period in separate experimental groups. KT-362 produced a reduction in heart rate (HR) and the HR-systolic pressure product. Mean arterial pressure (MAP) was reduced during occlusion and early reperfusion in the KT-362-treated group, and segment function (% segment shortening) was improved during the first hour of reperfusion. As compared with the control group, KT-362 produced a marked reduction in myocardial infarct size.[3]

别名	KT 362, KT362, KT-362
分子量	516.61
分子式	C26H32N2O7S
CAS No.	105394-80-7

存储

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

溶解度

DMSO: 5.16 mg/mL (10 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9357 mL	9.6785 mL	19.357 mL	48.3924 mL
	5 mM	0.3871 mL	1.9357 mL	3.8714 mL	9.6785 mL
	10 mM	0.1936 mL	0.9678 mL	1.9357 mL	4.8392 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

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参考文献

1. Cheng YN, et al. Effects of KT-362, a new antiarrhythmic agent, on membrane ionic currents of guinea pig ventricular myocytes. J Pharmacol Exp Ther. 1994;270(3):851-857. 2. Tatsukawa Y, et al. Effects of KT-362, a sarcolemmal and intracellular calcium antagonist, on calcium transients of cultured neonatal rat ventricular cells: a comparison with gallopamil and ryanodine. Cardiovasc Drugs Ther. 1997;10(6):667-675. 3. Pelc LR, et al. Reduction of myocardial ischemia-reperfusion injury by KT-362, a new intracellular calcium antagonist in anesthetized dogs. J Cardiovasc Pharmacol. 1989;13(4):586-593. 4. Ueyama N, et al. Change of mechanical activity to contraction from the relaxation induced by the intracellular Ca2+ antagonist KT-362; effects of alkylation of side chain, and substitution of 2,3,4,5-tetrahydro-1,5-benzothiazepine derivatives. Chem Pharm Bull (Tokyo). 1997;45(11):1761-1766. 5. Erker T. Studies on the chemistry of thieno-annealed O,N- and S,N-containing heterocyclics. 9. Synthesis and calcium channel blocking action of theino-analogs of KT-362. Arch Pharm (Weinheim). 1995;328(4):313-316. 6. Farber NE, et al. Cardioprotective effects of a new vascular intracellular calcium antagonist, KT-362, in the stunned myocardium. J Pharmacol Exp Ther. 1989;248(1):39-43. 7. Pieper GM, et al. Augmented vascular relaxation to KT-362 in diabetic rat aorta: comparison to diltiazem. J Cardiovasc Pharmacol. 1990;16(3):394-400. 8. Buljubasic N, et al. Comparative cardiac effects of KT-362 and verapamil in isolated heart--correlation to calcium channel current depression. J Cardiovasc Pharmacol. 1991;18(4):594-604.

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。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

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。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

KT-362 fumarate 105394-80-7 Membrane transporter/Ion channel Metabolism Potassium Channel Calcium Channel Sodium Channel KT 362 KT362 KT362 Fumarate KT-362 KT-362 Fumarate KT 362 Fumarate Inhibitor inhibitor inhibit

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KT-362 fumarate

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords