Falipamil

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MedKoo CAT#: 328018

CAS#: 77862-92-1

Description: Falipamil, also known as AQ-A-39, is a calcium channel antagonist potentially for the treatment of ischaemic heart disorder and sinus. Falipamil (AQ-A 39) is also a verapamil derivative which exerts antitachycardic effects by a direct action on the sinus node. Falipamil decreases HR at exercise in normal subjects and may exert antianginal effects in patients with myocardial ischemia. Falipamil exhibits effects on the electrical activity of the heart, reflecting the predominant direct vagolytic effect of this drug.

Chemical Structure

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Falipamil
CAS# 77862-92-1
Instruction

Theoretical Analysis

MedKoo Cat#: 328018
Name: Falipamil
CAS#: 77862-92-1
Chemical Formula: C24H32N2O5
Exact Mass: 428.23
Molecular Weight: 428.529
Elemental Analysis: C, 67.27; H, 7.53; N, 6.54; O, 18.67

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: Falipamil; AQ-A-39; AQ-A 39; AQ-A39.

IUPAC/Chemical Name: 2-(3-((3,4-dimethoxyphenethyl)(methyl)amino)propyl)-5,6-dimethoxyisoindolin-1-one

InChi Key: UUMGNNQOCVDZDG-UHFFFAOYSA-N

InChi Code: InChI=1S/C24H32N2O5/c1-25(12-9-17-7-8-20(28-2)21(13-17)29-3)10-6-11-26-16-18-14-22(30-4)23(31-5)15-19(18)24(26)27/h7-8,13-15H,6,9-12,16H2,1-5H3

SMILES Code: O=C1N(CCCN(CCC2=CC=C(OC)C(OC)=C2)C)CC3=C1C=C(OC)C(OC)=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:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 428.53 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.

Recalculate based on batch purity %
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:
In vitro protocol:
In vivo protocol:

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1: Boucher M, Chassaing C, Chapuy E. Cardiac electrophysiological effects of falipamil in the conscious dog: comparison with alinidine. Eur J Pharmacol. 1996 Jun 13;306(1-3):93-8. PubMed PMID: 8813620.

2: Boucher M, Chassaing C, Chapuy E, Duchêne-Marullaz P. Chronotropic cardiac effects of falipamil in conscious dogs: interactions with the autonomic nervous system and various ionic conductances. J Cardiovasc Pharmacol. 1994 Apr;23(4):569-75. PubMed PMID: 7516006.

3: Ilias W, Lackner F, Zimpfer M. [The intraoperative use of falipamil (AQ-A39), a new calcium antagonist with specific bradytropic properties]. Anaesthesist. 1990 Oct;39(10):487-92. German. PubMed PMID: 2278367.

4: Roth W, Koss FW, Hallinan D, Lambe R, Darragh A. Pharmacokinetics of falipamil after intravenous administration to humans. J Pharm Sci. 1990 May;79(5):415-9. PubMed PMID: 2352161.

5: Naudascher M, Jaillon P, Lecocq B, Lecocq V, Ferry A, Hilaire J, Maria JF. Effects of falipamil (AQ-A 39) on heart rate and blood pressure in resting and exercising healthy volunteers. J Cardiovasc Pharmacol. 1989 Jul;14(1):1-5. PubMed PMID: 2475699.

6: Takeda M, Furukawa Y, Ogiwara Y, Saegusa K, Haniuda M, Akahane K, Chiba S. Effects on atrio-ventricular conduction of alinidine and falipamil injected into the AV node artery of the anesthetized dog. Arch Int Pharmacodyn Ther. 1989 Jan-Feb;297:39-48. PubMed PMID: 2730241.

7: Ogiwara Y, Furukawa Y, Akahane K, Haniuda M, Chiba S. Bradycardic effects of AQ-A 39 (falipamil) in situ and in isolated, blood-perfused dog hearts. Comparison with alinidine and verapamil. Jpn Heart J. 1988 Nov;29(6):849-61. PubMed PMID: 3241338.

8: Huemer G, Hlozanek C, Lackner F, Niederle B, Schernthaner G, Schwarz S, Ilias W, Zimpfer M. [Falipamil for decreasing intraoperative heart rate in pheochromocytoma]. Acta Med Austriaca. 1988;15(4):103-5. German. PubMed PMID: 3213376.

9: Gülker H. A summary of the acute effects of falipamil in man. Eur Heart J. 1987 Dec;8 Suppl L:141-6. Review. PubMed PMID: 3330525.

10: Lévy S, Mètge M, Hilaire J, Cointe R, Bru P, Eychenne JL, Gérard R. Electrophysiologic properties of falipamil (AQA-39)--a new bradycardiac agent. Eur Heart J. 1987 Nov;8(11):1236-40. PubMed PMID: 3691560.

11: Tryba M, Zenz M. [Therapy of perioperative sinus tachycardia with the new calcium antagonist falipamil]. Arzneimittelforschung. 1987 Nov;37(11):1298-300. German. PubMed PMID: 3440040.

12: Gross GJ, Daemmgen JW. Effect of the new specific bradycardia agent AQ-A39 (falipamil) on coronary collateral blood flow in dogs. J Cardiovasc Pharmacol. 1987 Jul;10(1):123-7. PubMed PMID: 2441148.

13: Gross GJ, Daemmgen JW. Beneficial effects of two specific bradycardic agents AQ-A39 (falipamil) and AQ-AH 208 on reversible myocardial reperfusion damage in anesthetized dogs. J Pharmacol Exp Ther. 1986 Aug;238(2):422-8. PubMed PMID: 3735124.