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SKA-121

Name: SKA-121
Brand: TargetMol
SKU: T16891
Rating: 4.5 (1 reviews)

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Catalog No. T16891Cas No. 1820708-73-3

SKA-121 is a selective KCa3.1 activator (EC50s: 109 nM and 4.4 μM for KCa3.1 and KCa2.3, respectively).

SKA-121

😃Good

Catalog No. T16891Cas No. 1820708-73-3

SKA-121 is a selective KCa3.1 activator (EC50s: 109 nM and 4.4 μM for KCa3.1 and KCa2.3, respectively).

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
2 mg	$82	5 days	5 days
1 mL x 10 mM (in DMSO)	$86	5 days	5 days

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Product Introduction

Bioactivity

Description	SKA-121 is a selective KCa3.1 activator (EC50s: 109 nM and 4.4 μM for KCa3.1 and KCa2.3, respectively).
Targets&IC50	KCa3.1:（EC50）109 nM, KCa2.3:4.4 μM（EC50）
In vitro	SKA-121 is a typical positive-gating modulator and shifts the calcium-concentration response curve of KCa3.1 to the left. SKA-121 shows 41-fold selectivity for KCa3.1 (EC50 109 nM±14 nM) over KCa2.3 (EC50 4.4 ± 1.6 μM). SKA-121 is 200- to 400-fold selective over representative KV (KV1.3, KV2.1, KV3.1, and KV11.1), NaV (NaV1.2, NaV1.4, NaV1.5, and NaV1.7), as well as CaV1.2 channels [1].
In vivo	SKA-121 is relatively well soluble (logP=1.79) and can potentially be added to drinking water in animal experiments, it orally is also administered, and find that it has an oral availability of roughly 25%. SKA-121 has a short half-life (~20 minutes), and plasma decay is extremely rapid (21.3±2.4 μM at 5 minutes; 483±231 nM at 1 hour and 53±44 nM at 4 hours). SKA-121 can be used as a new KCa3.1 selective pharmacological tool compound despite its relatively short half-life in mice. SKA-121 (100 mg/kg i.p.) significantly lowers mean arterial blood pressure in normotensive and hypertensive wild-type but not in KCa3.1-/- mice in blood pressure telemetry experiments. A lower dose of SKA-121(30 mg/kg) does not produce significant alterations in the MAP [1].

Chemical Properties

Molecular Weight	198.22
Formula	C₁₂H₁₀N₂O
Cas No.	1820708-73-3
Smiles	Cc1cc2nc(N)oc2c2ccccc12
Relative Density.	1.302 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 42.86 mg/mL (216.22 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	5.0449 mL	25.2245 mL	50.4490 mL	252.2450 mL
5 mM	1.0090 mL	5.0449 mL	10.0898 mL	50.4490 mL
10 mM	0.5045 mL	2.5224 mL	5.0449 mL	25.2245 mL
20 mM	0.2522 mL	1.2612 mL	2.5224 mL	12.6122 mL
50 mM	0.1009 mL	0.5045 mL	1.0090 mL	5.0449 mL
100 mM	0.0504 mL	0.2522 mL	0.5045 mL	2.5224 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc