1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. Calcium Channel
  3. Diltiazem

Diltiazem 

Cat. No.: HY-B0632
Handling Instructions

Diltiazem is an orally active L-type Ca2+ channel blocker, with antihypertensive and antiarrhythmic effects. Diltiazem can be used for the research of cardiac arrhythmia, hypertension, and angina pectoris.

For research use only. We do not sell to patients.

Diltiazem Chemical Structure

Diltiazem Chemical Structure

CAS No. : 42399-41-7

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Description

Diltiazem is an orally active L-type Ca2+ channel blocker, with antihypertensive and antiarrhythmic effects. Diltiazem can be used for the research of cardiac arrhythmia, hypertension, and angina pectoris[1][2][3].

IC50 & Target

L-type Ca2+ channel[1]

In Vitro

Diltiazem (200 µM) in the superfusate, multichannel currents shows a use-dependent decline in amplitude reflecting reductions in the numbers of superpositions of channel openings in isolated guinea pig ventricular myocytes[1].
Diltiazem 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.

In Vivo

Diltiazem (100 mg/kg; p.o.; for 4 weeks) prevents aortic aneurysm formation in a blood pressure-independent manner[3].
Diltiazem limits aortic aneurysm formation in mice by a blood pressure–independent anti-inflammatory effect on monocytic cells[3].
Diltiazem (2 mg/kg; i.v.) has t1/2 of 61.2 min, CLel of 3.2 mL/min[4].

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

Animal Model: Male ApoE−/− mice, angiotensin II induced aneurysms[3]
Dosage: 100 mg/kg
Administration: Oral administration, in drinking water, for 4 weeks
Result: Srongly reduced the vascular remodeling but also lowered the blood pressure.
Animal Model: Rat (200-250 g)[4]
Dosage: 2 mg/kg (Pharmacokinetic Analysis)
Administration: Intravenous injection
Result: T1/2 (61.2 min), CLel (3.2 mL/min)
Molecular Weight

414.52

Formula

C₂₂H₂₆N₂O₄S

CAS No.

42399-41-7

SMILES

CN(C)CCN1C2=CC=CC=C2S[[email protected]@H](C3=CC=C(OC)C=C3)[[email protected]@H](OC(C)=O)C1=O

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Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

DiltiazemCalcium ChannelCa2+ channelsCa channelsantihypertensiveantiarrhythmiccardiacarrhythmiahypertensionanginapectorisInhibitorinhibitorinhibit

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