1448754-43-5

Basic information

• Product Name: Eleclazine (hydrochloride)
• Synonyms: Eleclazine (hydrochloride);1,4-Benzoxazepin-5(2H)-one, 3,4-dihydro-4-(2-pyrimidinylmethyl)-7-[4-(trifluoromethoxy)phenyl]-, hydrochloride (1:1)
• CAS NO: 1448754-43-5
• Molecular Formula: C₂₁H₁₆F₃N₃O₃*ClH
• Molecular Weight: 451.8261896
• Mol File: 1448754-43-5.mol
• Article Data: 2

Chemical Properties

• Appearance: /
• CAS DataBase Reference: Eleclazine (hydrochloride)(CAS DataBase Reference)
• NIST Chemistry Reference: Eleclazine (hydrochloride)(1448754-43-5)
• EPA Substance Registry System: Eleclazine (hydrochloride)(1448754-43-5)

Safety Data

• Hazardous Substances Data: 1448754-43-5(Hazardous Substances Data)

Usage

General Description

Eleclazine hydrochloride is a drug that belongs to a class of medications known as cardiac ion channel blockers. It works by blocking the ion channels in the heart that are responsible for regulating the heart's rhythm. This can help to prevent abnormal heart rhythms, such as those that can occur in conditions like atrial fibrillation. Eleclazine hydrochloride may be prescribed to help regulate irregular heartbeats in patients with certain types of arrhythmias. It is typically taken orally, and the dosage and administration of the drug will be determined by a healthcare provider based on the individual patient's medical history and condition. As with any medication, Eleclazine hydrochloride can potentially cause side effects, so it should be taken only under the supervision of a doctor.

Upstream product

• 1443211-72-0 4-(pyrimidin-2-ylmethyl)-7-(4-(trifluoromethoxy)phenyl)-3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-one 
• 49660-57-3 6-bromochroman-4-one 
• 5755-05-5 7-bromo-3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-one 

Relevant articles and documents

Discovery of Dihydrobenzoxazepinone (GS-6615) Late Sodium Current Inhibitor (Late INai), a Phase II Agent with Demonstrated Preclinical Anti-Ischemic and Antiarrhythmic Properties

Late sodium current (late INa) is enhanced during ischemia by reactive oxygen species (ROS) modifying the Nav 1.5 channel, resulting in incomplete inactivation. Compound 4 (GS-6615, eleclazine) a novel, potent, and selective inhibitor of late INa, is currently in clinical development for treatment of long QT-3 syndrome (LQT-3), hypertrophic cardiomyopathy (HCM), and ventricular tachycardia-ventricular fibrillation (VT-VF). We will describe structure-activity relationship (SAR) leading to the discovery of 4 that is vastly improved from the first generation late INa inhibitor 1 (ranolazine). Compound 4 was 42 times more potent than 1 in reducing ischemic burden in vivo (S-T segment elevation, 15 min left anteriorior descending, LAD, occlusion in rabbits) with EC50 values of 190 and 8000 nM, respectively. Compound 4 represents a new class of potent late INa inhibitors that will be useful in delineating the role of inhibitors of this current in the treatment of patients.