Pilsicainide HCl
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MedKoo CAT#: 329454

CAS#: 88069-49-2 (HCl)

Description: Pilsicainide, also known as SUN 1165, is a drug used clinically in Japan to treat cardiac arrhythmias. It functions by blocking the fast inward movement of sodium ions through the Nav1.5 sodium channel that contributes to the rapid depolarization characteristic of phase 0 in the cardiac action potential. Pilsicainide is a pure sodium channel blocker, meaning it does not significantly affect any other cardiac channels including potassium and calcium channels.


Price and Availability

Size
Price

1g
USD 250
10g
USD 850
100g
USD 2950
Size
Price

2g
USD 350
20g
USD 1250
200g
USD 5650
Size
Price

5g
USD 550
50g
USD 1950

Pilsicainide hydrochloride, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide). Shipping fee: from $30.00 (USA); from $45.00 (Canada); from $70.00 (international).


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 329454
Name: Pilsicainide HCl
CAS#: 88069-49-2 (HCl)
Chemical Formula: C17H25ClN2O
Exact Mass:
Molecular Weight: 308.85
Elemental Analysis: C, 66.11; H, 8.16; Cl, 11.48; N, 9.07; O, 5.18


Synonym: Pilsicainide hydrochloride; SUN 1165; SUN-1165; SUN1165.

IUPAC/Chemical Name: N-(2,6-dimethylphenyl)-2-(tetrahydro-1H-pyrrolizin-7a(5H)-yl)acetamide hydrochloride

SMILES Code: O=C(NC1=C(C)C=CC=C1C)CC23CCCN2CCC3.[H]Cl


Technical Data

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).

Harmonized System Code:
293490


Additional Information

Related CAS#
88069-49-2 (Pilsicainide hydrochloride)
88069-67-4 (Pilsicainide free base)


References

1: Yamasaki H, Tada H, Sekiguchi Y, Aonuma K. Right coronary cusp as a new window of ablation for pilsicainide-induced ventricular premature contractions in a patient with Brugada syndrome. Heart Vessels. 2016 Aug;31(8):1397-401. doi: 10.1007/s00380-015-0760-3. PubMed PMID: 26510553.

2: Shimizu M, Hashiguchi M, Shiga T, Nakamura K, Tamura HO, Mochizuki M. Quantitation of pilsicainide in microscale samples of human biological fluids using liquid chromatography-tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2015 Mar 15;985:172-9. doi: 10.1016/j.jchromb.2015.01.013. PubMed PMID: 25687803.

3: Nakatani S, Taniike M, Makino N, Egami Y, Shutta R, Tanouchi J, Nishino M. A Case of Sudden Cardiac Death due to Pilsicainide-Induced Torsades de Pointes. Korean Circ J. 2014 Mar;44(2):122-4. doi: 10.4070/kcj.2014.44.2.122. PubMed PMID: 24653743; PubMed Central PMCID: PMC3958607.

4: Qiu Q, Liu W, Li J, Wei Y, Yang K, Suo W, Wu W, Du H, Zhang Y, Zhao G, Zhou Z, Zheng Y, Lin Y. Pharmacokinetics of pilsicainide hydrochloride for injection in healthy Chinese volunteers: a randomized, parallel-group, open-label, single-dose study. Clin Ther. 2014 Feb 1;36(2):255-63. doi: 10.1016/j.clinthera.2013.12.015. PubMed PMID: 24480637.

5: Nakamura K, Fukami N. Altered responses to vasopressors of a patient medicated with carvedilol, pilsicainide and enalapril. J Anesth. 2014 Aug;28(4):625-7. doi: 10.1007/s00540-013-1762-x. PubMed PMID: 24366327.

6: Takahara A, Suzuki S, Hagiwara M, Nozaki S, Sugiyama A. Electrophysiological effects of an anti-influenza drug oseltamivir on the guinea-pig atrium: comparison with those of pilsicainide. Biol Pharm Bull. 2013;36(10):1650-2. PubMed PMID: 24088258.

7: Takahara A, Takeda K, Tsuneoka Y, Hagiwara M, Namekata I, Tanaka H. Electrophysiological effects of the class Ic antiarrhythmic drug pilsicainide on the guinea-pig pulmonary vein myocardium. J Pharmacol Sci. 2012;118(4):506-11. PubMed PMID: 22466963.

8: Kaneko Y, Nakajima T, Kato T, Kurabayashi M. Pilsicainide-induced polymorphic ventricular tachycardia. Intern Med. 2012;51(4):443-4. PubMed PMID: 22333385.

9: Fukuda K, Watanabe J, Yagi T, Wakayama Y, Nakano M, Kondo M, Kumagai K, Miura M, Shirato K, Shimokawa H. A sodium channel blocker, pilsicainide, produces atrial post-repolarization refractoriness through the reduction of sodium channel availability. Tohoku J Exp Med. 2011;225(1):35-42. PubMed PMID: 21869589.

10: Kajimoto K, Imai T, Minami Y, Kasanuki H. Comparison of acute reduction in left ventricular outflow tract pressure gradient in obstructive hypertrophic cardiomyopathy by disopyramide versus pilsicainide versus cibenzoline. Am J Cardiol. 2010 Nov 1;106(9):1307-12. doi: 10.1016/j.amjcard.2010.06.059. PubMed PMID: 21029829.

11: Desaphy JF, Dipalma A, Costanza T, Bruno C, Lentini G, Franchini C, George A, Conte Camerino D. Molecular determinants of state-dependent block of voltage-gated sodium channels by pilsicainide. Br J Pharmacol. 2010 Jul;160(6):1521-33. doi: 10.1111/j.1476-5381.2010.00816.x. PubMed PMID: 20590641; PubMed Central PMCID: PMC2938822.

12: Plosker GL. Pilsicainide. Drugs. 2010 Mar 5;70(4):455-67. doi: 10.2165/11204960-000000000-00000. Review. PubMed PMID: 20205487.

13: Iwasaki H, Takahara A, Nakamura Y, Satoh Y, Nagai T, Shinkai N, Sugiyama A. Simultaneous assessment of pharmacokinetics of pilsicainide transdermal patch and its electropharmacological effects on atria of chronic atrioventricular block dogs. J Pharmacol Sci. 2009 Jul;110(3):410-4. PubMed PMID: 19574726.

14: Chinushi M, Tagawa M, Izumi D, Furushima H, Aizawa Y. Pilsicainide-induced ST segment elevation and ST segment depression in two patients with variant forms of Brugada-type electrocardiographic abnormalities. Pacing Clin Electrophysiol. 2009 Jun;32(6):811-5. doi: 10.1111/j.1540-8159.2009.02371.x. PubMed PMID: 19545347.

15: Kim BH, Kim JR, Lim KS, Kim JW, Kim KP, Hong JH, Jang IJ, Shin SG, Yu KS, Tanaka T. An open-label, single-dose, parallel-group, dose-increasing study comparing the pharmacokinetics and tolerability of pilsicainide hydrochloride in healthy Korean and Japanese male subjects. Clin Ther. 2009 Mar;31(3):609-18. doi: 10.1016/j.clinthera.2009.03.015. PubMed PMID: 19393851.

16: Horiuchi D, Iwasa A, Sasaki K, Owada S, Kimura M, Sasaki S, Okumura K. Effect of pilsicainide on dominant frequency in the right and left atria and pulmonary veins during atrial fibrillation: association with its atrial fibrillation terminating effect. Eur J Pharmacol. 2009 Apr 17;608(1-3):54-61. doi: 10.1016/j.ejphar.2009.02.040. PubMed PMID: 19268659.

17: Oe K, Nagata M, Mori K. Pilsicainide intoxication presenting as left ventricular dyssynchrony in a patient on hemodialysis. J Cardiol. 2009 Feb;53(1):136-9. doi: 10.1016/j.jjcc.2008.07.002. PubMed PMID: 19167649.

18: Komatsu T, Tachibana H, Sato Y, Ozawa M, Ohshima K, Orii M, Kunigida F, Nakamura M. A randomized study on the efficacy of intravenous cibenzoline and pilsicainide administered prior to electrical cardioversion in patients with lone paroxysmal and persistent atrial fibrillation. J Cardiol. 2009 Feb;53(1):35-42. doi: 10.1016/j.jjcc.2008.08.007. PubMed PMID: 19167636.

19: Hikiji W, Kudo K, Nishida N, Ishida T, Usumoto Y, Tsuji A, Ikeda N. Acute fatal poisoning with pilsicainide and atenolol. Int J Legal Med. 2008 Nov;122(6):503-6. doi: 10.1007/s00414-008-0269-8. PubMed PMID: 18642016.

20: Ueyama T, Shimizu A, Esato M, Yoshiga Y, Sawa A, Suzuki S, Sugi N, Matsuzaki M. Pilsicainide-induced Brugada-type ECG and ventricular arrhythmias originating from the left posterior fascicle in a case with Brugada syndrome associated with idiopathic left ventricular tachycardia. Europace. 2008 Jan;10(1):86-90. PubMed PMID: 18037690.