Nicainoprol | CAS-924 | RU-42924 | CAS#76252-06-7 | calcium channel antagonist

MedKoo Cat#: 328013 | Name: Nicainoprol

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Nicainoprol, also known as CAS-924; RU-42924, is calcium channel antagonist and a putative class I antiarrhythmic agent. Nicainoprol could be useful in the prevention and treatment of arrhythmias associated with acute myocardial infarction.

Chemical Structure

Nicainoprol

CAS#76252-06-7

Theoretical Analysis

MedKoo Cat#: 328013

Name: Nicainoprol

CAS#: 76252-06-7

Chemical Formula: C21H27N3O3

Exact Mass: 369.2052

Molecular Weight: 369.47

Elemental Analysis: C, 68.27; H, 7.37; N, 11.37; O, 12.99

Price and Availability

Size	Price	Availability
50mg	USD 250.00	2 Weeks
100mg	USD 450.00	2 Weeks
200mg	USD 750.00	2 Weeks
500mg	USD 1,550.00	2 Weeks
1g	USD 2,450.00	2 Weeks
2g	USD 3,950.00	2 Weeks
5g	USD 5,950.00	2 Weeks

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Related CAS #

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Synonym

Nicainoprol; CAS-924; RU-42924; CAS924; RU42924.

IUPAC/Chemical Name

1,2,3,4-Tetrahydro-8-(2-hydroxy-3-(isopropylamino)propoxy)-1-nicotinoylquinoline

InChi Key

AUIHHZBJBKRDIE-UHFFFAOYSA-N

InChi Code

InChI=1S/C21H27N3O3/c1-15(2)23-13-18(25)14-27-19-9-3-6-16-8-5-11-24(20(16)19)21(26)17-7-4-10-22-12-17/h3-4,6-7,9-10,12,15,18,23,25H,5,8,11,13-14H2,1-2H3

SMILES Code

O=C(N1CCCC2=C1C(OCC(O)CNC(C)C)=CC=C2)C3=CN=CC=C3

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

Nicainoprol is a fast-sodium-channel blocking drug, which is a potent antiarrhythmic agent.

In vitro activity:

This study examined the effects of nicainoprol (1-50 microM), a new antiarrhythmic agent, on the transmembrane action potentials in isolated papillary muscles of the guinea pig. Nicainoprol (greater than or equal to 5 microM) produced dose-dependent decreases in the maximal upstroke velocity (Vmax) of the action potential. Reference: J Cardiovasc Pharmacol. 1989 May;13(5):767-73. https://pubmed.ncbi.nlm.nih.gov/2472526/

In vivo activity:

In isolated working rat hearts nicainoprol (10(-6) M, 5 X 10(-6) M and 10(-5) M) induced concentration-related protection against reperfusion arrhythmia without changing the cardiodynamics, with the exception of a decrease in heart rate at the highest concentration. Given to anesthetized rats, nicainoprol (5 and 10 mg/kg i.v.) reduced dose dependently in the early post occlusion (0-30 min) period, the percentage of animals with premature ventricular complexes (PVCs) and ventricular tachycardia while completely preventing the occurrence of ventricular fibrillation. Reference: Eur J Pharmacol. 1987 Nov 17;143(3):391-401. https://pubmed.ncbi.nlm.nih.gov/3691662/

	Solvent	mg/mL	mM	comments
Solubility
	DMSO	29.0	78.49

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 369.47 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Kimura T, Imanishi S, Arita M. Electrophysiologic effects of nicainoprol, a putative class I antiarrhythmic agent, on the guinea pig ventricular papillary muscle. J Cardiovasc Pharmacol. 1989 May;13(5):767-73. PMID: 2472526. 2. Hashimoto K, Akiyama K, Mitsuhashi H. Antiarrhythmic effect of a new class 1 antiarrhythmic drug, nicainoprol, on canine ventricular arrhythmias. Jpn J Pharmacol. 1989 Feb;49(2):245-54. doi: 10.1254/jjp.49.245. PMID: 2733262. 3. Martorana PA, Linz W, Göbel H, Petry P, Schölkens BA. Effects of nicainoprol on reperfusion arrhythmia in the isolated working rat heart and on ischemia and reperfusion arrhythmia and myocardial infarct size in the anesthetized rat. Eur J Pharmacol. 1987 Nov 17;143(3):391-401. doi: 10.1016/0014-2999(87)90463-8. PMID: 3691662.

In vitro protocol:

In vivo protocol:

1. Hashimoto K, Akiyama K, Mitsuhashi H. Antiarrhythmic effect of a new class 1 antiarrhythmic drug, nicainoprol, on canine ventricular arrhythmias. Jpn J Pharmacol. 1989 Feb;49(2):245-54. doi: 10.1254/jjp.49.245. PMID: 2733262. 2. Martorana PA, Linz W, Göbel H, Petry P, Schölkens BA. Effects of nicainoprol on reperfusion arrhythmia in the isolated working rat heart and on ischemia and reperfusion arrhythmia and myocardial infarct size in the anesthetized rat. Eur J Pharmacol. 1987 Nov 17;143(3):391-401. doi: 10.1016/0014-2999(87)90463-8. PMID: 3691662.

1: Pacini DJ, Boachie-Ansah G, Kane KA. Modification by hypoxia, hyperkalaemia and acidosis of the cardiac electrophysiological effects of a range of antiarrhythmic drugs. Br J Pharmacol. 1992 Nov;107(3):665-70. PubMed PMID: 1472965; PubMed Central PMCID: PMC1907770. 2: Schneider W, Reifart N, Blaeser A, Ostrowski J, Kaltenbach M, Kober G. Dose-related antiarrhythmic effects of nicainoprol in patients with chronic ventricular arrhythmias--a double-blind, placebo-controlled, cross-over multicentre trial. Nicainoprol Study Group. Eur Heart J. 1991 Aug;12(8):900-8. PubMed PMID: 1915428. 3: Hashimoto K, Sugiyama A, Haruno A, Matsuzaki T, Hirasawa A. Effects of a new antiarrhythmic drug TYB-3823 on canine ventricular arrhythmia models. J Cardiovasc Pharmacol. 1991 Feb;17(2):336-42. PubMed PMID: 1709241. 4: Sen S, Rettig G, Heisel A, Ozbek C, Schieffer H. Electrophysiological effects of nicainoprol in patients with paroxysmal supraventricular tachycardias. Int J Cardiol. 1990 Nov;29(2):221-7. PubMed PMID: 2269541. 5: Linz W, Schölkens BA, Kaiser J, Just M, Qi BY, Albus U, Petry P. Cardiac arrhythmias are ameliorated by local inhibition of angiotensin formation and bradykinin degradation with the converting-enzyme inhibitor ramipril. Cardiovasc Drugs Ther. 1989 Dec;3(6):873-82. PubMed PMID: 2535056. 6: Weirich J, Antoni H. Modelling frequency- and voltage-dependent effects of a class I antiarrhythmic drug (nicainoprol) on Vmax of the cardiac action potential from guinea-pig papillary muscle. Naunyn Schmiedebergs Arch Pharmacol. 1989 Oct;340(4):456-64. PubMed PMID: 2586635. 7: Hashimoto K, Ishii M, Watanabe K. Relationships between ventricular arrhythmias and plasma concentrations of ME3202 (CM7857) in dogs. J Cardiovasc Pharmacol. 1989 Jul;14(1):121-6. PubMed PMID: 2475703. 8: Kimura T, Imanishi S, Arita M. Electrophysiologic effects of nicainoprol, a putative class I antiarrhythmic agent, on the guinea pig ventricular papillary muscle. J Cardiovasc Pharmacol. 1989 May;13(5):767-73. PubMed PMID: 2472526. 9: Hashimoto K, Akiyama K, Mitsuhashi H. Antiarrhythmic effect of a new class 1 antiarrhythmic drug, nicainoprol, on canine ventricular arrhythmias. Jpn J Pharmacol. 1989 Feb;49(2):245-54. PubMed PMID: 2733262. 10: Weirich J, Antoni H. Evaluation and interpretation of voltage- and frequency-dependent electrophysiologic effects of a new class I antiarrhythmic agent (nicainoprol) on guinea pig papillary muscle and isolated heart. J Cardiovasc Pharmacol. 1988 Dec;12(6):664-71. PubMed PMID: 2467084. 11: Sen S, Rettig G, Schieffer H, Bette L. [Dose-related effect of nicainoprol (CAS 924) on basic electrophysiologic parameters in patients with and without diseases of the heart conduction system]. Z Kardiol. 1988 Sep;77(9):600-7. German. PubMed PMID: 3195179. 12: Libersa CC, Caron JF, Kacet S, Dagano J, Vincent A, Dupuis B, Gayet JL, Lekieffre JP. Electrophysiological effects of intravenous nicaïnoprol, a new antiarrhythmic agent, in 11 patients. Eur Heart J. 1988 Mar;9(3):271-8. PubMed PMID: 3383868. 13: Martorana PA, Linz W, Göbel H, Petry P, Schölkens BA. Effects of nicainoprol on reperfusion arrhythmia in the isolated working rat heart and on ischemia and reperfusion arrhythmia and myocardial infarct size in the anesthetized rat. Eur J Pharmacol. 1987 Nov 17;143(3):391-401. PubMed PMID: 3691662. 14: Ishizaki T, Horai Y, Kubota K, Minegishi A, Echizen H, Chiba K. Disposition kinetics and dynamics of nicainoprol, a new antiarrhythmic agent, in humans. Clin Pharmacol Ther. 1987 Nov;42(5):525-34. PubMed PMID: 3677541. 15: Horai Y, Ishizaki T. Determination of nicainoprol, a new antiarrhythmic agent, in human plasma and urine by high-performance liquid chromatography. J Chromatogr. 1986 Nov 28;383(1):103-10. PubMed PMID: 3818828. 16: Sen S, Rettig G, Ozbek C, Fröhlig G, Schieffer H, Bette L. Electrophysiological effects of a new antiarrhythmic agent, nicainoprol, in humans. J Cardiovasc Pharmacol. 1986 Jan-Feb;8(1):144-50. PubMed PMID: 2419677.