Molecular Formula | C11H8N2S |
Molar Mass | 200.26 |
Density | 1.403±0.06 g/cm3(Predicted) |
Melting Point | 184-188°C |
Boling Point | 417.1±28.0 °C(Predicted) |
Appearance | morphological solid |
pKa | 3.50±0.30(Predicted) |
Storage Condition | Keep in dark place,Sealed in dry,2-8°C |
Physical and Chemical Properties | EPA Chemical Information Naphtho[1,2-d]thiazol-2-amine (40172-65-4) |
Hazard Symbols | Xn - Harmful |
Risk Codes | R20/21/22 - Harmful by inhalation, in contact with skin and if swallowed. R36/37/38 - Irritating to eyes, respiratory system and skin. R36 - Irritating to the eyes R22 - Harmful if swallowed |
Safety Description | S22 - Do not breathe dust. S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection. S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 4.994 ml | 24.968 ml | 49.935 ml |
5 mM | 0.999 ml | 4.994 ml | 9.987 ml |
10 mM | 0.499 ml | 2.497 ml | 4.994 ml |
5 mM | 0.1 ml | 0.499 ml | 0.999 ml |
solubility | DMSO: ≥30mg/mL |
biological activity
SKA-31 is an activator of potassium ion channel (potassium channel). the EC50 values of KCa3.1,KCa2.2,KCa2.1 and KCa2.3 are 260 nM,1.9 μM,2.9 μM and 2.9 μM respectively, which can enhance endothelial hyperpolarization factor response and reduce blood pressure.
target
EC50: 2.9 μM (KCa2.1), 1.9 μM (KCa2.2), 2.9 μM (KCa2.3), 260 nM (KCa3.1)
in vitro study
SKA-31 activates KCa2/3 channels more potently than PK 26124, and is more selective over other Ion channels.
SKA-31 reduces cell viability with IC 50s of 5.3 μM , 46.9 μM in HCT-116 cells and HCT-8 cells, respectively.
SKA-31 (5.3 μM; 0-96 hours) reduces HCT-116 cells proliferation when added at time zero at 5.3 μM.
SKA-31 triggers apoptosis in HCT-116 cells at 5 μM, and the effect is smaller in HCT-8 cells at 45 μM.
SKA-31 increases the percentage of cells in G0/G1 phase in HCT-116 and HCT-8 cell lines at 5 μM and 45 μM, respectively.
SKA-31 further activates Caspase 3 and reduces Akt phosphorylation induced by CDDP.
SKA-31 has a synergic effect with CDDP also on the inhibition of HCT-116 cell proliferation.
in vivo studies
SKA-31 is not acutely toxic and has good pharmacokinetic properties.
SKA-31 potentiates native KCa3.1 and KCa2.3 in murine carotid endothelium with EC 50 values of 225 nM and 1.6 μM for KCa3.1 and KCa2.3, respectively.
SKA-31 stimulates KCa3.1 and KCa2.3 in vascular endothelial cells and increases acetylcholine-induced endothelium-derived hyperpolarizing factor (EDHF) -mediated vasodilation.
SKA-31 potentiates EDHF-type vasodilations and lowers blood pressure in mice. Injections of SKA-31 (1-30 mg/kg; I .p.) lower MAP over 24 hours in normotensive wild-type mice but not in KCa3.1(-/-) mice (-/-).