Diltiazem hydrochloride

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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:

33286-22-5

包装与价格：

包装	价格(元)
10 mM * 1 mL in Water	电议
500mg	电议
1 g	电议
5 g	电议
10 g	电议
50 g	电议

产品名称

盐酸地尔硫卓
CRD-401

产品介绍

Diltiazem hydrochloride是钙离子流入抑制剂（缓慢通道阻断剂或钙拮抗剂）。

生物活性

Diltiazem hydrochloride is aCa²⁺influx inhibitor (slow channel blocker or calcium antagonist).

体外研究
(In Vitro)

Benzothiazepine Ca²⁺antagonist diltiazem hydrochloride interacts with transmembrane segments IIIS6 and IVS6 in the α1 subunit of L-type Ca²⁺channels^[1]. Diltiazem causes a dose-dependent inhibiton of contractions as well as Ca²⁺influx stimulated by alpha adrenoceptor activation and high-K⁺depolarization. Diltiazem is roughly equally potent in inhibiting contractions induced by high-K⁺and a low concentration of norepinephrine (NE)^[2]. Diltiazem also inhibits the Na-dependent Ca-efflux from heart mitochondria. Both the (+)-optical isomers of the cis- and trans-forms of diltiazem inhibit Na-Ca exchange activity with comparable potency (IC₅₀of 10-20 μM)^[3].

体内研究
(In Vivo)

Diltiazem produces a noncompetitive inhibition of Ca²⁺-induced contractions of depolarized rabbit aorta. Furthermore, there is a lack of parallelism between the smooth muscle effects of removal of [Ca²⁺]ex and of addition of diltiazem^[2]. Diltiazem improves the cardiac microcirculation and function in an experimental model of hyperthyroidism in rats. The treatment of hyperthyroid rats with losartan diltiazem (4.7±0.7%; P< 0.001) significantly reduces the percentage of fibrosis areas in the left ventricle^[4]. In conscious spontaneously hypertensive rats (SHR), diltiazem dose-dependently decreases the blood pressure and increases the heart rate after intravenous administration (0.03--1 mg/kg). Oral administration of diltiazem (100 mg/kg) also reduces the blood pressure of SHR^[5].

Clinical Trial

分子量

450.98

性状

Solid

Formula

C₂₂H₂₇ClN₂O₄S

CAS 号

33286-22-5

中文名称

盐酸地尔硫卓

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

H₂O : 33.33 mg/mL(73.91 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.2174 mL	11.0870 mL	22.1739 mL
5 mM	0.4435 mL	2.2174 mL	4.4348 mL
10 mM	0.2217 mL	1.1087 mL	2.2174 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.
请依序添加每种溶剂： PBS
Solubility: 100 mg/mL (221.74 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在本网站选购。