Art. -Nr.: HY-107414

SKA-121

3 Cited Publications

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Based on 3 publication(s) in Google Scholar

SKA-121 is a selective K_Ca3.1 activator. SKA-121 exhibits EC₅₀s of 109 nM and 4.4 μM for K_Ca3.1 and K_Ca2.3, respectively.

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Reinheit: 99.69%
CAS. Nr.: 1820708-73-3
Formel: C₁₂H₁₀N₂O
Molecular Weight:198.22

Speicherung:

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

SKA-121 Chemical Structure

CAS. Nr.: 1820708-73-3

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

SKA-121 is a selective K_Ca3.1 activator. SKA-121 exhibits EC₅₀s of 109 nM and 4.4 μM for K_Ca3.1 and K_Ca2.3, respectively.

IC₅₀ & Target

EC50: 109 nM (K_Ca3.1), 4.4 μM (K_Ca2.3)^[1]

In Vitro

SKA-121, a compound generated through an isosteric replacement approach. SKA-121 is a typical positive-gating modulator and shifts the calcium-concentration response curve of K_Ca3.1 to the left. SKA-121 displays 41-fold selectivity for K_Ca3.1 (EC₅₀ 109 nM±14 nM) over K_Ca2.3 (EC₅₀ 4.4 ± 1.6 μM). SKA-121 is 200- to 400-fold selective over representative K_V (K_V1.3, K_V2.1, K_V3.1, and K_V11.1), Na_V (Na_V1.2, Na_V1.4, Na_V1.5, and NaV1.7), as well as Ca_V1.2 channels^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In blood pressure telemetry experiments, SKA-121 (100 mg/kg i.p.) significantly lowers mean arterial blood pressure in normotensive and hypertensive wild-type but not in K_Ca3.1^-/- mice. SKA-121 can be used as a new K_Ca3.1 selective pharmacological tool compound despite its relatively short half-life in mice. A lower dose of 30 mg/kg of SKA-121 does not produce significant alterations in MAP. The vehicle, peanut oil/DMSO (9:1 v/v, for SKA-121), does not cause significant alterations in MAP or HR. 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). Since 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%^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 1820708-73-3
Appearance Solid
Molecular Weight 198.22
Formel C₁₂H₁₀N₂O
Color White to gray
SMILES

NC1=NC2=CC(C)=C3C=CC=CC3=C2O1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (3)

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Int J Mol Sci

Transcriptional Repression of CCL2 by KCa3.1 K+ Channel Activation and LRRC8A Anion Channel Inhibition in THP-1-Differentiated M2 Macrophages. [Abstract]

2025 Aug 6;26(15):7624. PMID: 40806751
Int J Mol Sci

Downregulation of IL-8 and IL-10 by LRRC8A Inhibition through the NOX2-Nrf2-CEBPB Transcriptional Axis in THP-1-Derived M2 Macrophages. [Abstract]

2024 Sep 5;25(17):9612. PMID: 39273558
Int J Mol Sci

Downregulation of IL-8 and IL-10 by the Activation of Ca2+-Activated K+ Channel KCa3.1 in THP-1-Derived M2 Macrophages. [Abstract]

2022 Aug 3;23(15):8603. PMID: 35955737

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 42.86 mg/mL (216.22 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

5.0449 mL

25.2245 mL

50.4490 mL

5 mM

1.0090 mL

5.0449 mL

10.0898 mL

10 mM

0.5045 mL

2.5224 mL

5.0449 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Protokoll

Kinase Assay^[1]

To fully evaluate the selectivity of the naphthooxazole SKA-121, seven-point concentration-response curves on K_Ca2.1, K_Ca2.2, K_Ca2.3 and K_Ca3.1 are determined with 250 nM free Ca²⁺ in the internal solution^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

Mice^[1]
Twelve-week-old male C57Bl/6J mice are used. For i.v. application, SKA-121 is dissolved at 5 mg/mL in a mixture of 10% CremophorEL and 90% phosphate-buffered saline and then injected at 10 mg/kg into the tail vein (n=8 mice per compound). Another group of mice (n=8) receive SKA-121 orally. At various time points after the injection, blood is collected into EDTA blood sample collection tubes either from the saphenous vein or by cardiac puncture under deep isoflurane anesthesia. After the cardiac puncture, mice are sacrificed by cutting the heart, and then the brain is removed. Individual mice are typically used for three times points (two blood collections from the saphenous vein plus the terminal blood collection).

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Coleman N, et al. New positive Ca2+-activated K+ channel gating modulators with selectivity for KCa3.1. Mol Pharmacol. 2014 Sep;86(3):342-57. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	5.0449 mL	25.2245 mL	50.4490 mL	126.1225 mL
	5 mM	1.0090 mL	5.0449 mL	10.0898 mL	25.2245 mL
	10 mM	0.5045 mL	2.5224 mL	5.0449 mL	12.6122 mL
	15 mM	0.3363 mL	1.6816 mL	3.3633 mL	8.4082 mL
	20 mM	0.2522 mL	1.2612 mL	2.5224 mL	6.3061 mL
	25 mM	0.2018 mL	1.0090 mL	2.0180 mL	5.0449 mL
	30 mM	0.1682 mL	0.8408 mL	1.6816 mL	4.2041 mL
	40 mM	0.1261 mL	0.6306 mL	1.2612 mL	3.1531 mL
	50 mM	0.1009 mL	0.5045 mL	1.0090 mL	2.5224 mL
	60 mM	0.0841 mL	0.4204 mL	0.8408 mL	2.1020 mL
	80 mM	0.0631 mL	0.3153 mL	0.6306 mL	1.5765 mL
	100 mM	0.0504 mL	0.2522 mL	0.5045 mL	1.2612 mL

Keywords

SKA-121

3 Cited Publications

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SKA-121

Membrane Transporter/Ion Channel Compound Library

Anti-Cardiovascular Disease Compound Library

Neuroprotective Compound Library

Targeted Diversity Library

Potassium Channel Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Activators Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) SKA-121

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SKA-121

Membrane Transporter/Ion Channel Compound Library

Anti-Cardiovascular Disease Compound Library

Neuroprotective Compound Library

Targeted Diversity Library

Potassium Channel Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Activators Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) SKA-121

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SKA-121 Related Classifications

HY-107414 Related Classifications