Diltiazem

Research use only, not for human use.

Diltiazem (CRD 401 free base) is an orally available L-type Ca2+ channel blocker with antihypertensive, antiarrhythmic, and cardioprotective properties that prevent post-reperfusion myocardial injury, angina pectoris, and cardiovascular-related diseases.

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

Diltiazem (200 μM) elicits a use-dependent blockade that proceeded within a relatively small number of pulses.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.

Diltiazem (100 mg/kg; p.o.; for 4 weeks) prevents aortic aneurysm formation in a blood pressure-independent manner.Diltiazem limits aortic aneurysm formation in mice by a blood pressure-independent anti-inflammatory effect on monocytic cells. Diltiazem (2 mg/kg; i.v.) exhibits T1/2 of 61.2 min, CLel of 3.2 mL/min in rats.Animal Model:Male ApoE?/? mice, angiotensin II induced aneurysms 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) Dosage:2 mg/kg (Pharmacokinetic Analysis) Administration:Intravenous injection Result:T1/2 (61.2 min), CLel (3.2 mL/min)

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GPCR/G Protein

Calcium Channel

Calcium Channel

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42399-41-7

414.52

C22H26N2O4S

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (120.62 mM; Ultrasonic ) H2O : < 0.1 mg/mL (insoluble)

O(C(C)=O)[C@@H]1[C@@H](SC=2C(N(CCN(C)C)C1=O)=CC=CC2)C3=CC=C(OC)C=C3

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(-20℃)

With Ice Pack

≥ 2 years