Diltiazem HCl

SKU: orb1310926

Description

Diltiazem hydrochloride is a benzothiazepine-class calcium channel antagonist that inhibits calcium ion influx, resulting in vasodilation. It is widely used in cardiovascular research, including in vitro electrophysiology studies and in vivo models of hypertension and angina.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 33286-22-5
• MW: 450.98
• Purity: >98%
• Formula: C₂₂H₂₆N₂O₄S  HCl
• SMILES: Cl.COc1ccc(cc1)[C@@H]1Sc2ccccc2N(CCN(C)C)C(=O)[C@@H]1OC(C)=O
• Target: Ion channel
• Solubility: Soluble in DMSO (up to 45 mg/ml) or in Water (up to 50 mg/ml)

Bioactivity

• 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.
• In Vitro:
  Benzothiazepine Ca2+ antagonist diltiazem hydrochloride interacts with transmembrane segments IIIS6 and IVS6 in the α1 subunit of L-type Ca2+ channels. 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). 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).

Storage & Handling

• Storage: RT
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Ca2+ channels, Ca channels, Calcium Channel, CRD 401, CRD401, CRD-401, Diltiazem, Diltiazem HCl, Diltiazem Hydrochloride, Diltiazem hydrochloride, CalciumChannel, Inhibitor, inhibit, RG 83606 HCl

Compound Identifiers

PubChem CID

62920