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MedChemExpress - Model Diltiazem malate ...

MedChemExpress - Model Diltiazem malate - 144604-00-2

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

MCE China：Diltiazem malate

Brand：MedChemExpress (MCE)

Cat. No.HY-B0632A

CAS：144604-00-2

Synonyms：MK 793

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

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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.

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].

IC50 & Target：L-type calcium channel

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. [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]

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
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•   The biological activity of the products has been verified by the experiments of customers in various countries；
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