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SKA-121

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).

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

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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).
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

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 42.86 mg/mL (216.22 mM)

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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DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

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