Diltiazem

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Diltiazem

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

42399-41-7

地尔硫卓

Diltiazem 是一种口服 L 型钙通道 (L-type Ca²⁺channel) 阻滞剂。 Diltiazem 具有抗高血压和抗心律失常作用。Diltiazem 可用于心律失常、高血压和心绞痛的研究。

生物活性

Diltiazem is an orally activeL-type Ca²⁺channelblocker. Diltiazem shows 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]

体外研究
(In Vitro)

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

体内研究
(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.) exhibits T_1/2of 61.2 min, CL_elof 3.2 mL/min in rats^[4].

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:	T_1/2(61.2 min), CL_el(3.2 mL/min)

Clinical Trial

分子量

414.52

Formula

C₂₂H₂₆N₂O₄S

CAS 号

42399-41-7

中文名称

地尔硫卓

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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