| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
| Targets |
SKA-31 targets small and intermediate conductance calcium-activated potassium channels (KCa2.x and KCa3.1). It is a positive modulator that enhances channel activity by increasing their sensitivity to calcium. By activating these channels, it promotes K⁺ efflux and membrane hyperpolarization, which reduces cellular excitability. This mechanism underlies its blood pressure-lowering effects and its ability to modulate neuronal activity. The compound shows a preference for KCa3.1 over KCa2 channels, with EC50 values of 260 nM for KCa3.1, 1.9 μM for KCa2.2, 2.9 μM for KCa2.1, and 2.9 μM for KCa2.3.
|
|---|---|
| ln Vitro |
More specifically than other ion channels, SKA-31 inhibits KCa2/3 channels and activates them more effectively than PK 26124 [1]. In HCT-116 cells and HCT-8 cells, the IC50 values for SKA-31 are 5.3 μM and 46.9 μM, respectively [2]. SKA-31 (5.3 μM; 0-96 hours) decreases the swelling of HCT-116 cells [2]. HCT-116 cells are activated by SKA-31 (5 μM), and SKA-31 at 45 μM raises the proportion of G0/G1 phase cells in HCT-116 and HCT-8 cell lines at concentrations of 5 μM and 45 μM, respectively[2]. SKA-31 decreases CDDP-induced Akt phosphorylation and increases Caspase 3 activation [2]. Additionally effective at preventing HCT-116 cell proliferation are SKA-31 and CDDP [2].
In vitro, SKA-31 is a potent activator of SK/IK channels. It activates KCa3.1 with an EC50 of 260 nM, KCa2.2 with an EC50 of 1.9 μM, KCa2.1 with an EC50 of 2.9 μM, and KCa2.3 with an EC50 of 2.9 μM. The compound's activity can be assessed using electrophysiological techniques such as patch-clamp. It is used to study the role of SK/IK channels in various cell types, including neurons, endothelial cells, and smooth muscle cells. It is a valuable tool for studying these channels and their physiological roles. |
| ln Vivo |
SKA-31 exhibits favorable pharmacokinetic characteristics and no acute effects [1]. SKA-31 activates KCa3.1 and KCa2.3 in vascular endothelial cells and increases myocardial choline Induced endothelium-derived epidermal hyperplatelet (EDHF)-mediated vasodilation [1]. It also enhances native KCa3.1 and KCa2.3 in carotid endothelial cells. 1.6 μM and 225 nM, in that order[1]. SKA-31 (1-30 mg/kg; ip) decreases glycemic MAP in normal wild-type mice during a 24-day period, but not KCa3.1. It also improves EDHF-type vasodilation and lowers glycemia in mice.
SKA-31 lowers blood pressure in vivo by activating SK/IK channels, which causes vasodilation and reduces vascular resistance. It can modulate neuronal activity, making it useful for studying neurological disorders. It is a valuable tool for studying the potential therapeutic applications of SK/IK channel activators in conditions such as hypertension, ataxia, and epilepsy. However, detailed published in vivo efficacy data are limited, and further studies are needed to fully characterize its therapeutic potential. |
| Enzyme Assay |
The in vitro assay for SKA-31 involves measuring its activation of SK/IK channels using electrophysiological techniques such as patch-clamp. Cells expressing KCa3.1, KCa2.1, KCa2.2, or KCa2.3 are treated with varying concentrations of SKA-31 (0.1 nM-100 µM), and the resulting potassium current is measured. The EC50 is calculated from dose-response curves. The compound's selectivity is confirmed by testing against other channels. The shift in the calcium-concentration response curve can be assessed by measuring channel activity at different calcium concentrations.
|
| Cell Assay |
Cell viability assay [2]
Cell Types: HCT-116 cells, HCT-8 cells Tested Concentrations: Incubation Duration: 24 hrs (hours) Experimental Results: Cell viability was diminished in HCT-116 and HCT-8, with IC50s of 5.3 μM and 46.9 μM respectively. Cell proliferation assay[2] Cell Types: HCT-116 Cell Tested Concentrations: 5.3 μM Incubation Duration: 0-96 hrs (hours) Experimental Results: HCT-116 cell proliferation diminished when IC50S value was added at time zero. Apoptosis analysis [2] Cell Types: HCT-116 cells, HCT-8 cells Tested Concentrations: 5 μM (HCT-116 cells), 45 μM (HCT-8 cells) Incubation Duration: 24 hrs (hours) Experimental Results: Triggered HCT-116 cells apoptosis, and the effect was smaller in HCT-8 cells. Cell cycle analysis[2] Cell Types: HCT-116 cells, HCT-8 Cell Tested Concentrations: 5 μM (HCT-116), 45 μM (HCT-8) Incubation Duration: 24 hrs (hours) Experimental Results: G0/% increase in cells HCT-116 and G1 phase of HCT-8 cell line. Western Blot Analysis [2] Cell Types: HCT-116 cells Tested Concentrations: Incubation Duration: 24 hrs (hours) Experimental Results: When HCT-116 cells were co-treated with CDDP, Caspase 3 was fur In vitro cellular assays for SKA-31 use cell lines expressing SK/IK channels, such as neurons, endothelial cells, or smooth muscle cells. Cells are treated with the compound at concentrations of 0.1 nM-100 µM. Membrane potential is measured using fluorescent dyes (e.g., DiBAC4(3)), and intracellular calcium is measured using Fluo-4 or Fura-2. Cell viability is assessed using MTT or CCK-8 assays. The compound's effects on cell proliferation, migration, and cytokine production can be evaluated. These assays help characterize the compound's mechanism of action as an SK/IK channel activator. |
| Animal Protocol |
Animal/Disease Models: 16-25 weeks of mice[1]
Doses: 1 mg/kg, 10 mg/kg, 30 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: -/-) Mouse (-/-) MAP[1] . Normotensive wild-type mice had lower MAP over 24 hrs (hrs (hours)), but not KCa3.1(-/-) mice(-/-). In vivo animal studies for SKA-31 involve mouse models of hypertension, ataxia, or epilepsy. The compound is administered via intraperitoneal or intravenous injection at doses of 0.1-10 mg/kg. Blood pressure is measured using tail-cuff or telemetry. Motor function is assessed using behavioral tests such as the rotarod or open field. Seizure activity is monitored in epilepsy models. The compound's effects on vascular tone and neuronal excitability are evaluated. However, detailed published in vivo data are limited. |
| ADME/Pharmacokinetics |
SKA-31 is a small molecule with good cell permeability. It has a molecular weight of approximately 196.27 and a molecular formula of C11H8N2S. It is soluble in DMSO and should be stored at -20°C for long-term preservation as a powder and at -80°C in solvent. Its pharmacokinetic properties, including oral bioavailability, half-life, and tissue distribution, are not extensively reported in the available literature. For in vivo studies, it can be formulated in suitable vehicles.
|
| References |
|
| Additional Infomation |
SKA-31 is a potassium channel activator with the CAS number 40172-65-4. It activates KCa3.1 (EC50 = 260 nM), KCa2.1 (2.9 μM), KCa2.2 (1.9 μM), and KCa2.3 (2.9 μM). It is a small molecule that lowers blood pressure and modulates neuronal activity. The compound is a research tool and is not for human therapeutic use.
|
| Molecular Formula |
C11H8N2S
|
|---|---|
| Molecular Weight |
200.259
|
| Exact Mass |
200.041
|
| CAS # |
40172-65-4
|
| PubChem CID |
94880
|
| Appearance |
Gray to brown solid powder
|
| Density |
1.403g/cm3
|
| Boiling Point |
417.1ºC at 760 mmHg
|
| Melting Point |
184-188ºC
|
| Flash Point |
206.1ºC
|
| Index of Refraction |
1.83
|
| LogP |
3.612
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
0
|
| Heavy Atom Count |
14
|
| Complexity |
221
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
FECQXVPRUCCUIL-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C11H8N2S/c12-11-13-10-8-4-2-1-3-7(8)5-6-9(10)14-11/h1-6H,(H2,12,13)
|
| Chemical Name |
benzo[e][1,3]benzothiazol-2-amine
|
| Synonyms |
SKA31 SKA 31 SKA-31
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~624.19 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (12.48 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (12.48 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 2.08 mg/mL (10.39 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.9935 mL | 24.9675 mL | 49.9351 mL | |
| 5 mM | 0.9987 mL | 4.9935 mL | 9.9870 mL | |
| 10 mM | 0.4994 mL | 2.4968 mL | 4.9935 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
