PA-6 | CAS#500715-03-7

MedKoo Cat#: 531397 | Name: PA-6

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Description:

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

PA-6 is a selective and potent IK1 (inward rectifier potassium current) inhibitor that terminates atrial fibrillation and does not cause ventricular arrhythmias in goat and dog models. PA-6 interacts with the cytoplasmic pore region of the KIR2.1 (KCNJ2) ion channel.

Chemical Structure

PA-6

CAS#500715-03-7

Theoretical Analysis

MedKoo Cat#: 531397

Name: PA-6

CAS#: 500715-03-7

Chemical Formula: C31H32N4O2

Exact Mass: 492.2525

Molecular Weight: 492.62

Elemental Analysis: C, 75.58; H, 6.55; N, 11.37; O, 6.50

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Synonym

PA-6

IUPAC/Chemical Name

1,5-Bis[4-[[imino(phenyl)methyl]amino]phenoxy]pentane

InChi Key

PETGITKEGWIZEL-UHFFFAOYSA-N

InChi Code

InChI=1S/C31H32N4O2/c32-30(24-10-4-1-5-11-24)34-26-14-18-28(19-15-26)36-22-8-3-9-23-37-29-20-16-27(17-21-29)35-31(33)25-12-6-2-7-13-25/h1-2,4-7,10-21H,3,8-9,22-23H2,(H2,32,34)(H2,33,35)

SMILES Code

N=C(NC1=CC=C(OCCCCCOC2=CC=C(NC(C3=CC=CC=C3)=N)C=C2)C=C1)C4=CC=CC=C4

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

>3 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:

IK1 inhibitor PA-6 (PA-6), a pentamidine analogue, is a selective and potent IK1 (KIR2.x ion-channel-carried inward rectifier current) inhibitor, with IC50 values of 12-15 nM for human and mouse KIR2.x currents.

In vitro activity:

This study analysed seven pentamidine analogues (PA-1 to PA-7) for IK₁ blocking potency at 200 nM using inside-out patches from KIR2.1 expressing HEK-293 cells. PA-6 showed the highest potency and was tested further. PA-6 blocked KIR2.x currents of human and mouse with low IC₅₀ values (12-15 nM). Modelling indicated that PA-6 had less electrostatic but more lipophilic interactions with the cytoplasmic channel pore than P, resulting in a higher channel affinity for PA-6 (ΔG -44.1 kJ/Mol) than for P (ΔG -31.7 kJ/Mol). Reference: Cardiovasc Res. 2013 Jul 1;99(1):203-14. https://pubmed.ncbi.nlm.nih.gov/23625347/

In vivo activity:

PA-6 was applied i.v. in anaesthetized goats with rapid pacing-induced AF and anaesthetized dogs with chronic atrio-ventricular (AV) block. PA-6 (2.5 mg·kg-1 ·10 min-1 ) induced cardioversion to sinus rhythm (SR) in 5/6 goats and prolonged AF cycle length. AF complexity decreased significantly before cardioversion. PA-6 accumulated in cardiac tissue with ratios between skeletal muscle : atrial muscle : ventricular muscle of approximately 1:8:21. Reference: Br J Pharmacol. 2017 Aug;174(15):2576-2590. https://pubmed.ncbi.nlm.nih.gov/28542844/

	Solvent	mg/mL	mM
Solubility
	DMSO	125.0	253.74

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 492.62 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. Takanari H, Nalos L, Stary-Weinzinger A, de Git KC, Varkevisser R, Linder T, Houtman MJ, Peschar M, de Boer TP, Tidwell RR, Rook MB, Vos MA, van der Heyden MA. Efficient and specific cardiac IK₁ inhibition by a new pentamidine analogue. Cardiovasc Res. 2013 Jul 1;99(1):203-14. doi: 10.1093/cvr/cvt103. Epub 2013 Apr 25. PMID: 23625347. 2. Ji Y, Varkevisser R, Opacic D, Bossu A, Kuiper M, Beekman JDM, Yang S, Khan AP, Dobrev D, Voigt N, Wang MZ, Verheule S, Vos MA, van der Heyden MAG. The inward rectifier current inhibitor PA-6 terminates atrial fibrillation and does not cause ventricular arrhythmias in goat and dog models. Br J Pharmacol. 2017 Aug;174(15):2576-2590. doi: 10.1111/bph.13869. Epub 2017 Jun 28. PMID: 28542844; PMCID: PMC5513871.

In vitro protocol:

In vivo protocol:

1. Ji Y, Varkevisser R, Opacic D, Bossu A, Kuiper M, Beekman JDM, Yang S, Khan AP, Dobrev D, Voigt N, Wang MZ, Verheule S, Vos MA, van der Heyden MAG. The inward rectifier current inhibitor PA-6 terminates atrial fibrillation and does not cause ventricular arrhythmias in goat and dog models. Br J Pharmacol. 2017 Aug;174(15):2576-2590. doi: 10.1111/bph.13869. Epub 2017 Jun 28. PMID: 28542844; PMCID: PMC5513871.

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