144604-00-2

144604-00-2 structure

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)
Chemical 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 Formula: C₂₆H₃₂N₂O₉S
Molecular Weight: 548.60500
Catalog: Signaling Pathways Membrane Transporter/Ion Channel Calcium Channel
Create Date: 2018-06-12 18:49:51
Modify Date: 2024-01-12 14:38:09
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].

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)

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	Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel Research Areas >> Cardiovascular Disease
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.

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

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