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

Diltiazem hydrochloride (Synonyms: CRD-401)

Cat. No.: HY-14656 Purity: 99.83%
Handling Instructions

Diltiazem hydrochloride is a Ca2+ influx inhibitor (slow channel blocker or calcium antagonist).

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

Diltiazem hydrochloride Chemical Structure

Diltiazem hydrochloride Chemical Structure

CAS No. : 33286-22-5

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Based on 2 publication(s) in Google Scholar

Other Forms of Diltiazem hydrochloride:

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Description

Diltiazem hydrochloride is a Ca2+ influx inhibitor (slow channel blocker or calcium antagonist).

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 (IC50 of 10-20 μM)[3].

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

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].

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

Molecular Weight

450.98

Formula

C₂₂H₂₇ClN₂O₄S

CAS No.

33286-22-5

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

DiltiazemCRD-401CRD401CRD 401Calcium ChannelCa2+ channelsCa channelsInhibitorinhibitorinhibit

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Product Name:
Diltiazem hydrochloride
Cat. No.:
HY-14656
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