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KT-362 fumarate

Catalog No. T27753 CAS 105394-80-7

Synonyms: KT 362, KT362, KT-362

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.

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KT-362 fumarate, CAS 105394-80-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 323.00
5 mg	In stock	$ 747.00
10 mg	In stock	$ 1,050.00
25 mg	In stock	$ 1,560.00
50 mg	In stock	$ 2,080.00
100 mg	In stock	$ 2,830.00
1 mL * 10 mM (in DMSO)	In stock	$ 897.00

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Purity: 99.90%

Purity: 99.87%

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Description	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.
In vitro	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]
In vivo	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]

Synonyms	KT 362, KT362, KT-362
Molecular Weight	516.61
Formula	C26H32N2O7S
CAS No.	105394-80-7

Storage

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

Solubility Information

DMSO: 5.16 mg/mL (10 mM)

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library Neuronal Signaling Compound Library Bioactive Compound Library Bioactive Compounds Library Max Anti-Cancer Compound Library

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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 inhibit

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