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Diltiazem hydrochloride

Catalog No. T0112 CAS 33286-22-5

Synonyms: CRD-401, RG 83606 HCl, Diltiazem HCl

Diltiazem hydrochloride (RG 83606 HCl) is a benzothiazepine calcium channel blocking agent with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions.

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Diltiazem hydrochloride Chemical Structure

Diltiazem hydrochloride, CAS 33286-22-5

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Purity: 99.65%

Purity: 99.52%

Purity: 98%

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Chemical Properties

Storage & Solubility Information

Description	Diltiazem hydrochloride (RG 83606 HCl) is a benzothiazepine calcium channel blocking agent with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions.
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].
In vivo	Diltiazem exhibits noncompetitive inhibition of calcium-induced contractions in depolarized rabbit aorta and lacks parallel effects between the removal of extracellular calcium ([Ca2+]ex) and its addition. It enhances cardiac microcirculation and function in hyperthyroid rat models, significantly reducing left ventricular fibrosis when combined with losartan (4.7±0.7%; P < 0.001). In spontaneously hypertensive rats, diltiazem lowers blood pressure and increases heart rate in a dose-dependent manner after intravenous administration (0.03--1 mg/kg) and through oral administration (100 mg/kg), demonstrating its therapeutic potential in hypertension management.

Synonyms	CRD-401, RG 83606 HCl, Diltiazem HCl
Molecular Weight	450.98
Formula	C22H27ClN2O4S
CAS No.	33286-22-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 100 mg/mL (221.74 mM)

DMSO: 12.4 mg/mL (27.5 mM)

References and Literature

1. Kraus RL, et al. Molecular mechanism of diltiazem interaction with L-type Ca2+ channels. J Biol Chem. 1998 Oct 16;273(42):27205-12. 2. van Breemen C, et al. The mechanism of inhibitory action of diltiazem on vascular smooth muscle contractility. J Pharmacol Exp Ther. 1981 Aug;218(2):459-63. 3. Chiesi M, et al. Stereospecific action of diltiazem on the mitochondrial Na-Ca exchange system and on sarcolemmal Ca-channels. Biochem Pharmacol. 1987 Sep 1;36(17):2735-40. 4. Freitas F, et al. Cardiac microvascular rarefaction in hyperthyroid rats is reversed by losartan, diltiazem, and propranolol. Fundam Clin Pharmacol. 2015 Feb;29(1):31-40. 5. Sato M, et al. Hypotensive effects of diltiazem hydrochloride in the normotensive, spontaneously hypertensive and renal hypertensive rats (author's transl). Nihon Yakurigaku Zasshi. 1979 Mar;75(2):99-106.

Related compound libraries

This product is contained In the following compound libraries：

Traditional Chinese Medicine Monomer Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Drug Repurposing Compound Library Membrane Protein-targeted Compound Library Cardiotoxicity Compound Library Bioactive Compounds Library Max Anti-Cardiovascular Disease Compound Library Orally Active Compound Library

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Keywords

Diltiazem hydrochloride 33286-22-5 Membrane transporter/Ion channel Metabolism Calcium Channel Inhibitor Diltiazem Ca channels CRD-401 inhibit RG 83606 HCl Diltiazem Hydrochloride CRD401 Ca2+ channels Diltiazem HCl CRD 401 inhibitor

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