Diltiazem malate  (Synonyms: 地尔硫卓苹果酸盐; MK 793)

Diltiazem malate is a potent and orally active L-type calcium channel 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].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 T_1/2 of 61.2 min, CL_el of 3.2 mL/min in rats^[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

548.61

C₂₆H₃₂N₂O₉S

144604-00-2

地尔硫卓苹果酸盐

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]