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| | Nifekalant hydrochloride Basic information |
| Product Name: | Nifekalant hydrochloride | | Synonyms: | 1,3-Dimethyl-6-[2-(N-(2-hydroxyethyl)-3-(4-nitrophenyl)propylamino)ethylamino]-2,4(1H,3H)-pyrimidinedione hydrochloride;Nifekalant 130636-43-0 /;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: | 130656-51-8 | | MF: | C19H28ClN5O5 | | MW: | 441.91 | | EINECS: | 1533716-785-6 | | Product Categories: | Inhibitors;Amines;Aromatics;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals | | Mol File: | 130656-51-8.mol |  |
| | Nifekalant hydrochloride Chemical Properties |
| Melting point | 172-174° | | storage temp. | Refrigerator | | solubility | DMSO (Slightly, Heated), Methanol (Slightly, Heated), Water (Slightly) | | form | Solid | | pka | 7.05(at 25℃) | | color | Light Yellow to Yellow | | CAS DataBase Reference | 130656-51-8(CAS DataBase Reference) |
| | Nifekalant hydrochloride Usage And Synthesis |
| Description | 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. | | Description | 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. | | Definition | ChEBI: Nifekalant hydrochloride is an amine. It contains a Nifekalant. | | Brand name | Shinbit |
| | Nifekalant hydrochloride Preparation Products And Raw materials |
| Raw materials | 3-(4-NITRO-PHENYL)-PROPAN-1-OL-->6-[N-(2-Hydroxyethyl)amino]-1,3-dimethyl-2,4(1H,3H)-dione-->6-Amino-1,3-dimethyl-1,2,3,4-tetrahydropyrimidine-2,4-dione-->2-(1,3-diMethyl-2,6-dioxo-1,2,3,6-tetrahydropyriMidin-4-ylaMino)ethyl 4-Methylbenzenesulfonate-->Nifekalant |
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