[CAS NO. 130656-51-8] Nifekalant hydrochloride

Name: Nifekalant hydrochloride
Brand: Arctom Scientific
SKU: AS359942

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PRODUCTS SPECIFICATIONS [130656-51-8]

Distributor

Catalog

AS359942

Brand

Arctom Scientific

CAS

130656-51-8

DESCRIPTION [130656-51-8]

Overview

MDL	MFCD00892243
Molecular Weight	441.91
Molecular Formula	C19H28ClN5O5
SMILES	[H]Cl.O=C1N(C)C(C=C(NCCN(CCO)CCCC2=CC=C([N+]([O-])=O)C=C2)N1C)=O

For research use only. We do not sell to patients.

Summary

Nifekalant hydrochloride (MS-551), a class III antiarrhythmic agent, is a IKr potassium channel blocker with an IC ₅₀ of 10 µM. Nifekalant hydrochloride can be used for refractory ventricular tachyarrhythmias research ^[1] ^[2] .

In Vitro

Nifekalant interacts with the cardiac M2 and the peripheral M3 receptors with a K _i value of 27 and 74 mM, respectively. Nifekalant dose dependently blocks HERG channels with an IC ₅₀ value of 7.9 mM, but Nifekalant does not block minK currents in the Xenopus oocyte expression system. Nifekalant blocks HERG channels mainly in their open state in a frequency dependent manner. As a pure K ⁺ channel blocker, Nifekalant does not have negative inotropic effects which amiodarone has via a β-blocking action and does not affect cardiac conduction ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In rats (a species deficient in functional cardiac IK), before coronary ligation, 3 mg/kg and 10 mg/kg MS-551 decreased the heart rate by 6% and 12%, and increased mean arterial pressure (MAP) by 14% and 33%, respectively. MS-551 prolongs the QT interval and reduced the incidence of sustained ventricular fibrillation (VF) after reperfusion ^[3] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT05169866	Beijing Anzhen Hospital	New Onset Atrial Fibrillation\|Complications; Cardiac, Postoperative	March 2022	Phase 3
NCT04209959	Second Affiliated Hospital of Nanchang University	Atrial Fibrillation	January 1, 2019	Phase 4
NCT03855826	Sichuan Baili Pharmaceutical Co., Ltd.	Ventricular Tachycardia\|Ventricular Fibrillation	January 15, 2019	Phase 4
NCT03853369	Sichuan Baili Pharmaceutical Co., Ltd.\|Peking University First Hospital\|Beijing Hospital	Ventricular Tachycardia\|Ventricular Fibrillation	February 18, 2019

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL ( 282.86 mM ; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2629 mL	11.3145 mL	22.6290 mL
5 mM	0.4526 mL	2.2629 mL	4.5258 mL
10 mM	0.2263 mL	1.1315 mL	2.2629 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (4.71 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (4.71 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (4.71 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

2,4(1H,3H)-Pyrimidinedione, 6-[[2-[(2-hydroxyethyl)[3-(4-nitrophenyl)propyl]amino]ethyl]amino]-1,3-dimethyl-, hydrochloride (1:1)

2,4(1H,3H)-Pyrimidinedione, 6-[[2-[(2-hydroxyethyl)[3-(4-nitrophenyl)propyl]amino]ethyl]amino]-1,3-dimethyl-, monohydrochloride

MS 551

Shinbit

Nifekalant hydrochloride