| Name | Diltiazem hydrochloride |
| 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | H2O : 100 mg/mL (221.74 mM), Sonication is recommended.
DMSO : 50 mg/mL (110.87 mM), Sonication is recommended.
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| Keywords | Inhibitor | inhibit | Diltiazem Hydrochloride | Diltiazem hydrochloride | Diltiazem | CRD401 | CRD 401 | CalciumChannel | Calcium Channel | Ca2+ channels | Ca channels |
| Inhibitors Related | Nisoldipine | Levetiracetam | L-Ascorbic acid | L-Phenylalanine | D-Menthol | Ethyl cinnamate | L-Ascorbic acid sodium salt | 1-Octanol | 2-Nitrobenzoic acid | Nifedipine | Methyl homoveratrate | Otilonium bromide |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | FDA-Approved Drug Library | Cosmetic Ingredient Compound Library | Bitter Compound library | Bioactive Compounds Library Max | Heat-Clearing and Detoxifying Traditional Chinese Medicine Compound Library |
United States
