ChemicalBook > CAS DataBase List > SKA-121

SKA-121

Product Name
SKA-121
CAS No.
1820708-73-3
Chemical Name
SKA-121
Synonyms
SKA-121;SKA121,SKA 121;Naphth[2,1-d]oxazol-2-amine, 5-methyl-;SKA-121 5-Methylnaphtho[2,1-d]oxazol-2-amin
CBNumber
CB74667080
Molecular Formula
C12H10N2O
Formula Weight
198.22
MOL File
1820708-73-3.mol
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SKA-121 Property

Boiling point:
403.2±38.0 °C(Predicted)
Density 
1.302±0.06 g/cm3(Predicted)
storage temp. 
2-8°C
solubility 
DMF: 50 mg/ml; DMSO: 50 mg/ml; DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml; Ethanol: 10 mg/ml
form 
powder
pka
4.48±0.30(Predicted)
color 
brown to dark gray
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML2206
Product name
SKA-121
Purity
≥98% (HPLC)
Packaging
5mg
Price
$91.8
Updated
2025/07/31
Sigma-Aldrich
Product number
SML2206
Product name
SKA-121
Purity
≥98% (HPLC)
Packaging
25mg
Price
$295
Updated
2025/07/31
Cayman Chemical
Product number
9003088
Product name
SKA-121
Purity
≥98%
Packaging
1mg
Price
$27
Updated
2024/03/01
Cayman Chemical
Product number
9003088
Product name
SKA-121
Purity
≥98%
Packaging
25 mg
Price
$565
Updated
2024/03/01
Cayman Chemical
Product number
9003088
Product name
SKA-121
Purity
≥98%
Packaging
500μg
Price
$43
Updated
2023/01/06
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SKA-121 Chemical Properties,Usage,Production

Uses

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.

Biochem/physiol Actions

SKA-121 is a KCa3.1 (IKCa1, IK1, KCa4, SKCa4, SK4) subtype-selective small conductance Ca2+-activated K+ channel (SK channel) positive-gating modulator (EC50 = 109 nM/KCa3.1 vs. 8.7 μM/KCa2.1, 6.8 μM/KCa2.2, 4.4 μM/KCa2.3) with 200- to 400-fold selectivity over CaV1.2 as well as representative KVs (KV1.3, KV2.1, KV3.1, and KV11.1) and NaV (NaV1.2, NaV1.4, NaV1.5, and NaV1.7) channels. When applied in vivo, SKA-121 significantly lowers mean arterial blood pressure in wild-type, but not KCa3.1(-/-), normotensive and hypertensive mice (100 mg/kg i.p.). SKA-121 is a more potent and selective KCa3.1 activator than SKA-31 (EC50 = 260 nM/KCa3.1, 2.9 μM/KCa2.1, 1.9 μM/KCa2.2, 2.9 μM/KCa2.3).

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].

storage

Store at -20°C

References

[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. DOI:10.1124/mol.114.093286

SKA-121 Preparation Products And Raw materials

Raw materials

Preparation Products

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SKA-121 Suppliers

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1820708-73-3, SKA-121Related Search:


  • SKA-121
  • Naphth[2,1-d]oxazol-2-amine, 5-methyl-
  • SKA-121 5-Methylnaphtho[2,1-d]oxazol-2-amin
  • SKA121,SKA 121
  • 1820708-73-3