2-Hydroxysuccinic acid-(2S,3S)-5-[2-(dimethylamino)ethyl]-2-(4- methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl a cetate (1:1)

Modify Date: 2024-01-12 14:38:09

2-Hydroxysuccinic acid-(2S,3S)-5-[2-(dimethylamino)ethyl]-2-(4- methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl a cetate (1:1) Structure
2-Hydroxysuccinic acid-(2S,3S)-5-[2-(dimethylamino)ethyl]-2-(4- methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl a cetate (1:1) structure
Common Name 2-Hydroxysuccinic acid-(2S,3S)-5-[2-(dimethylamino)ethyl]-2-(4- methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl a cetate (1:1)
CAS Number 144604-00-2 Molecular Weight 548.60500
Density N/A Boiling Point 594.4ºC at 760 mmHg
Molecular Formula C26H32N2O9S Melting Point N/A
MSDS N/A Flash Point 313.3ºC

 Use of 2-Hydroxysuccinic acid-(2S,3S)-5-[2-(dimethylamino)ethyl]-2-(4- methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl a cetate (1:1)


Diltiazem malate is a potent and orally active L-type calcium chanel inhibitor. Diltiazem malate shows antihypertensive and antiarrhythmic effects. Diltiazem malate can be used for the research of cardiac arrhythmia, hypertension, and angina pectoris[1][2][3].

 Names

Name 2-Hydroxysuccinic acid-(2S,3S)-5-[2-(dimethylamino)ethyl]-2-(4- methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl a cetate (1:1)

  Biological Activity

Description Diltiazem malate is a potent and orally active L-type calcium chanel inhibitor. Diltiazem malate shows antihypertensive and antiarrhythmic effects. Diltiazem malate can be used for the research of cardiac arrhythmia, hypertension, and angina pectoris[1][2][3].
Related Catalog
In Vitro Diltiazem malate (200 µM) elicits a use-dependent blockade that proceeded within a relatively small number of pulses[1].Diltiazem malate reduces Ca2+ influx by accelerating inactivation during action potentials, and that the use-dependent blockade is due to increases in the number of channels in a sustained closed state[1].
In Vivo Diltiazem malate (100 mg/kg; p.o.; daily for 4 weeks) prevents aortic aneurysm formation in a blood pressure-independent manner[3].Diltiazem malate (100 mg/kg; p.o.; daily for 6 days) with ATII (1.44 mg/kg; p.o.; daily for 6 days) reduces the ATII-induced vascular inflammation and macrophage accumulation in ApoE−/− mice[3].Diltiazem malate (2 mg/kg; i.v.) exhibits T1/2 of 61.2 min, CLel of 3.2 mL/min in rats[4].
References

[1]. Niimi Y, et al. Diltiazem facilitates inactivation of single L-type calcium channels in guinea pig ventricular myocytes. Jpn Heart J. 2003 Nov;44(6):1005-14.

[2]. S Lin Tang, et l. Structural Basis for Diltiazem Block of a Voltage-Gated Ca2+ Channel. Mol Pharmacol. 2019 Oct; 96(4): 485-492.

[3]. Mieth A, et al. L-type calcium channel inhibitor diltiazem prevents aneurysm formation by blood pressure-independent anti-inflammatory effects. Hypertension. 2013 Dec;62(6):1098-104.

[4]. S. J. Downing, et al. Diltiazem pharmacokinetics in the rat and relationship between its serum concentration and uterine and cardiovascular effects. Br J Pharmacol. 1987 Aug; 91(4): 735-745.

 Chemical & Physical Properties

Boiling Point 594.4ºC at 760 mmHg
Molecular Formula C26H32N2O9S
Molecular Weight 548.60500
Flash Point 313.3ºC
Exact Mass 548.18300
PSA 179.21000
LogP 2.34010
Vapour Pressure 4.27E-14mmHg at 25°C