IK1 inhibitor PA-6 (Synonyms: PA-6)

Name: IK1 inhibitor PA-6
Brand: MedChemExpress
SKU: HY-112544
Rating: 4.5 (1 reviews)

Cat. No.: HY-112544 Pureza: 99.29%: Ficha de datos
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IK1 inhibitor PA-6 (PA-6), a pentamidine analogue, is a selective and potent I_K1 (K_IR2.x ion-channel-carried inward rectifier current) inhibitor, with IC₅₀ values of 12-15 nM for human and mouse K_IR2.x currents. IK1 inhibitor PA-6 (PA-6) elevates K_IR2.1 protein expression and induces intracellular K_IR2.1 accumulation. IK1 inhibitor PA-6 (PA-6) has the potential to treat atrial fibrillation and arrhythmia.

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IK1 inhibitor PA-6 Estructura química

No. CAS : 500715-03-7

Tamaño	Stock	Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	Obtener un presupuesto
200 mg	Obtener un presupuesto

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Revisión del cliente

Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE IK1 inhibitor PA-6

•Nat Commun. 2022 Jun 21;13(1):3544. [Abstract]

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•Related Small Molecules:

•Related Proteins:

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Descripciòn

IC₅₀ & Target

IC50: 12-15 nM (K_IR2.x currents)^[1].

Peso molecular

492.61

Fòrmula

C₃₁H₃₂N₄O₂

No. CAS

500715-03-7

Appearance

Solid

Color

Off-white to light yellow

SMILES

N=C(C1=CC=CC=C1)NC2=CC=C(OCCCCCOC3=CC=C(NC(C4=CC=CC=C4)=N)C=C3)C=C2

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvente y solubilidad

In Vitro:

DMSO : 125 mg/mL (253.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0300 mL	10.1500 mL	20.3000 mL
5 mM	0.4060 mL	2.0300 mL	4.0600 mL
10 mM	0.2030 mL	1.0150 mL	2.0300 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculadora de molaridad
Calculadora de dilución

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.22 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.22 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.22 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Pureza y Documentación

Purity: 99.29%

Select Batch:

Ficha de datos (269 KB) SDS (251 KB)

COA (242 KB) HNMR (199 KB) LCMS (96 KB)

Instrucciones de manejo (2659 KB)

Referencias

[1]. Takanari H, et al. Efficient and specific cardiac IK₁ inhibition by a new pentamidine analogue. Cardiovasc Res. 2013 Jul 1;99(1):203-14. [Content Brief]

[2]. Ji Y, et al. 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. [Content Brief]

[3]. Ji Y, et al. PA-6 inhibits inward rectifier currents carried by V93I and D172N gain-of-function KIR2.1 channels, but increases channel protein expression. J Biomed Sci. 2017 Jul 15;24(1):44. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.0300 mL	10.1500 mL	20.3000 mL	50.7501 mL
	5 mM	0.4060 mL	2.0300 mL	4.0600 mL	10.1500 mL
	10 mM	0.2030 mL	1.0150 mL	2.0300 mL	5.0750 mL
	15 mM	0.1353 mL	0.6767 mL	1.3533 mL	3.3833 mL
	20 mM	0.1015 mL	0.5075 mL	1.0150 mL	2.5375 mL
	25 mM	0.0812 mL	0.4060 mL	0.8120 mL	2.0300 mL
	30 mM	0.0677 mL	0.3383 mL	0.6767 mL	1.6917 mL
	40 mM	0.0508 mL	0.2538 mL	0.5075 mL	1.2688 mL
	50 mM	0.0406 mL	0.2030 mL	0.4060 mL	1.0150 mL
	60 mM	0.0338 mL	0.1692 mL	0.3383 mL	0.8458 mL
	80 mM	0.0254 mL	0.1269 mL	0.2538 mL	0.6344 mL
	100 mM	0.0203 mL	0.1015 mL	0.2030 mL	0.5075 mL

IK1 inhibitor PA-6 Related Classifications

Cardiovascular Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

IK1 inhibitor PA-6500715-03-7PA-6PA6PA 6Potassium ChannelKcsAInhibitorinhibitorinhibit

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IK1 inhibitor PA-6 (Synonyms: PA-6)

Revisión del cliente

IK1 inhibitor PA-6 Related Antibodies

1 Publications Citing Use of MCE IK1 inhibitor PA-6

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Actividad biológica

Pureza y Documentación

Referencias

Revisión del cliente

Calculadora de molaridad

Calculadora de dilución

Complete Stock Solution Preparation Table

IK1 inhibitor PA-6 Related Classifications

Keywords:

Productos vistos recientemente:

Revisión del cliente

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report