2. Membrane Transporter/Ion Channel
  3. Potassium Channel
  4. SKA-121

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

For research use only. We do not sell to patients.

SKA-121 Chemical Structure

SKA-121 Chemical Structure

CAS No. : 1820708-73-3

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

SKA-121 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE SKA-121

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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

IC50 & Target

EC50: 109 nM (KCa3.1), 4.4 μM (KCa2.3)[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 KCa3.1 to the left. SKA-121 displays 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].

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

SKA-121 Related Antibodies
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 KCa3.1-/- mice. SKA-121 can be used as a new KCa3.1 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.
Molecular Weight

198.22

Formula

C12H10N2O
CAS No.
Appearance

Solid

Color

White to gray

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.0449 mL 25.2245 mL 50.4490 mL
5 mM 1.0090 mL 5.0449 mL 10.0898 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.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.64%

COA (253 KB) HNMR (173 KB) LCMS (517 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[1]

To fully evaluate the selectivity of the naphthooxazole SKA-121, seven-point concentration-response curves on KCa2.1, KCa2.2, KCa2.3 and KCa3.1 are determined with 250 nM free Ca2+ in the internal solution[1].

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).

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

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.

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
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SKA-121 Related Classifications

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:

SKA-1211820708-73-3SKA121SKA 121Potassium ChannelKcsAInhibitorinhibitorinhibit

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