130656-51-8

Basic information

• Product Name: Nifekalant hydrochloride
• Synonyms: Nifekalant 130636-43-0 /;1,3-Dimethyl-6-[2-(N-(2-hydroxyethyl)-3-(4-nitrophenyl)propylamino)ethylamino]-2,4(1H,3H)-pyrimidinedione hydrochloride;1,3-Dimethyl-6-((2-(N-(2-hydroxyethyl)-3-(4-nitrophenyl)propylamino)ethylamino)-2,4(1H),3H)-pyrimidinedione HCl;2,4(1H,3H)-Pyrimidinedione, 6-((2-((2-hydroxyethyl)(3-(4-nitrophenyl)propyl)amino)ethyl)amino)-1,3-dimethyl-, monohydrochloride;6-[[2-[(2-Hydroxyethyl)[3-(4-nitrophenyl)propyl]aMino]ethyl]aMino]-1,3-diMethyl-2,4(1H,3H)-pyriMidinedione Hydrochloride;Shinbit;ms551;NIFEKALANT HYDROCHLORIDE
• CAS NO: 130656-51-8
• Molecular Formula: C₁₉H₂₇N₅O₅*ClH
• Molecular Weight: 441.91
• EINECS: 1533716-785-6
• Product Categories: Amines;Aromatics;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Inhibitors
• Mol File: 130656-51-8.mol
• Article Data: 1

Chemical Properties

• Melting Point: 172-174°
• Boiling Point: 597.9 °C at 760 mmHg
• Flash Point: 315.4 °C
• Appearance: /
• Storage Temp.: Refrigerator
• Solubility: DMSO (Slightly, Heated), Methanol (Slightly, Heated), Water (Slightly)
• PKA: 7.05(at 25℃)
• CAS DataBase Reference: Nifekalant hydrochloride(CAS DataBase Reference)
• NIST Chemistry Reference: Nifekalant hydrochloride(130656-51-8)
• EPA Substance Registry System: Nifekalant hydrochloride(130656-51-8)

Safety Data

• Hazardous Substances Data: 130656-51-8(Hazardous Substances Data)

Usage

Description

Different sources of media describe the Description of 130656-51-8 differently. You can refer to the following data:
1. Nifekalant is a novel and pure class III anti-arrhythmic agent introduced in Japan as Shinbit injection for the treatment of serious ventricular arrhythmias. It can be synthesized in 3 steps with a final assembly of two ethanolamine blocks. Nifekalant is a non-selective blocker of myocardial repolarizing potassium currents and is completely devoid of any β-adrenergic blocking effect . In hearts from different species, Nifekalant significantly prolonged action potential duration, atrial and ventricular refractory periods in in situ and in isolation studies. In intact animals, hemodynamic parameters were not affected by doses up to 1 mg/kg. The specific characteristics of its voltage- and timedependent K+ current blockade might differentiate Nifekalant from other class III agents currently in use.
2. Nifekalant is a class III antiarrhythmic agent that has been shown to be beneficial to initial resuscitation after cardiac arrest in clinical trials. It blocks the rapidly activating delayed rectifier potassium channel (IKr; IC50 = 10 μM). Nifekalant is also inhibits the human multidrug and toxin extrusion (MATE) transporter 1 (MATE1; IC50 = 6.5 μM).

Chemical Properties

Yellow Solid

Originator

Mitsui (Japan)

Uses

Nifekalant Hydrochloride is a class III antiarrhythmic agent. Nifekalant Hydrochloride is used in the treatment of patients with extensive anterior infarction and severe ventricular dysfunction.

Brand name

Shinbit

InChI:InChI=1/C19H27N5O5.ClH/c1-21-17(14-18(26)22(2)19(21)27)20-9-11-23(12-13-25)10-3-4-15-5-7-16(8-6-15)24(28)29;/h5-8,14,20,25H,3-4,9-13H2,1-2H3;1H

Upstream product

• 130634-04-7 1,3-dimethyl-6-[2-(p-toluenesulfonyloxy)ethylamino)-2,4(1H,3H)-pyrimidinedione 
• 6642-31-5 6-Amino-1,3-dimethylbarbituric acid 
• 5770-44-5 6-(2-hydroxyethylamino)-1,3-dimethylpyrimidine-2,4(1H,3H)-dion 
• 130636-43-0 1,3-dimethyl-6-[2-(N-[2-hydroxyethyl]-3-[4-nitrophenyl]propylamino)ethylamino]-2,4(1H,3H)-pyrimidinedione 
• 20716-25-0 3-(4-nitrophenyl)-1-propanol 

Relevant articles and documents

A method for preparing high-purity hydrochloric acid Nepal non-Kalland

The invention discloses a preparation method of nifekalant hydrochloride. The preparation method comprises the following steps of: performing aminolysis on 6-imino-1,3-dimethyluracil to obtain 1,3-dimethyl-6-(2-ethoxy)aminouracil; esterfying 1,3-dimethyl-