| Identification | Back Directory | [Name]
SKA-121 | [CAS]
1820708-73-3 | [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 | [Molecular Formula]
C12H10N2O | [MDL Number]
MFCD31630822 | [MOL File]
1820708-73-3.mol | [Molecular Weight]
198.22 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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 |
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