SML2206

SKA-121

≥98% (HPLC)

• Synonym(e): 5-Methylnaphth[2,1-d]oxazol-2-amine, 5-Methylnaphtho[2,1-d]oxazol-2-amine, SKA 121, SKA121
• Empirische Formel (Hill-System): C₁₂H₁₀N₂O
• CAS-Nummer: 1820708-73-3
• Molekulargewicht: 198.22
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥98% (HPLC)
• Form: powder

Eigenschaften

• assay: ≥98% (HPLC)
• form: powder
• color: brown to dark gray
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: 2-8°C
• SMILES string: CC(C1=C2C=CC=C1)=CC3=C2OC(N)=N3
• InChI: 1S/C12H10N2O/c1-7-6-10-11(15-12(13)14-10)9-5-3-2-4-8(7)9/h2-6H,1H3,(H2,13,14)
• InChI key: JEGUERWMMMQFJV-UHFFFAOYSA-N

Beschreibung

Biochem/physiol Actions

KCa3.1 subtype-selective Ca2+-activated K+ channel activator with in vivo arterial blood pressure-lowering efficacy. More potent and selective than SKA-31.

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).

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable