| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg | |||
| 50mg | |||
| Other Sizes |
| Targets |
SKA-121 targets the intermediate-conductance calcium-activated potassium channel KCa3.1. It is a positive-gating modulator that binds to the channel and enhances its sensitivity to intracellular calcium. This leads to increased K⁺ efflux and membrane hyperpolarization. By shifting the calcium-concentration response curve of KCa3.1 to the left, SKA-121 facilitates channel opening at lower calcium concentrations. Its high selectivity for KCa3.1 over other channels makes it a valuable tool for studying the physiological role of this channel.
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| ln Vitro |
SKA-121, a substance made via isosteric substitution. A common positive gating modulator, SKA-121 causes KCa3.1's calcium concentration response curve to move to the left. Compared to KCa2.3 (EC50 4.4 ± 1.6 μM), SKA-121 exhibits a 41-fold increase in selectivity for KCa3.1 (EC50 109 nM±14 nM). Compared to representative KV (KV1.3, KV2.1, KV3.1, and KV11.1) and NaV (NaV1.2, NaV1.4, NaV1.5, and NaV1), SKA-121 exhibits 200–400 times higher selectivity. both CaV1.2 channels and 7 [1].
In vitro, SKA-121 is a potent and selective KCa3.1 activator. It exhibits an EC50 of 109 nM for KCa3.1 and displays 41-fold selectivity over KCa2.3 (EC50 = 4.4 µM). It shows 200- to 400-fold selectivity over representative KV, NaV, as well as CaV1.2 channels. As a positive-gating modulator, it shifts the calcium-concentration response curve of KCa3.1 to the left. These properties make it a highly selective tool for studying KCa3.1 function. |
| ln Vivo |
SKA-121 (100 mg/kg ip) dramatically lowered the mean arterial blood pressure in normotensive and hypertensive wild-type mice in blood pressure telemetry tests, but had no impact on KCa3.1-/- mice. Despite having a brief half-life in mice, SKA-121 has the potential to be a novel pharmacological tool that is selective for KCa3.1. SKA-121 at a lower dose of 30 mg/kg did not cause any appreciable MAP alterations. For SKA-121, the carrier peanut oil/DMSO (9:1 v/v) had no discernible effect on HR or MAP. The half-life of SKA-121 is roughly 20 minutes, and its plasma decays very quickly (21.3±2.4 μM at 5 minutes; 483±231 nM at 1 hour; 53±44 nM at 4 hours). Oral administration of SKA-121 is possible due to its relatively strong solubility (logP=1.79), which allows it to be added to drinking water in animal tests. Its oral utilization rate was determined to be roughly 25% [1].
SKA-121 can be used in vivo to study the role of KCa3.1 in regulating vascular tone and cellular excitability. By activating KCa3.1, it can cause vasodilation and modulate immune cell function. It is a valuable tool for studying the potential therapeutic applications of KCa3.1 modulators in conditions such as hypertension, asthma, inflammatory diseases, and neurological disorders. 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-121 involves measuring its activation of KCa3.1 channels using electrophysiological techniques such as patch-clamp. Cells expressing KCa3.1 are treated with varying concentrations of SKA-121 (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, including KCa2.3, KV, NaV, and CaV1.2. The shift in the calcium-concentration response curve is assessed by measuring channel activity at different calcium concentrations.
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| Cell Assay |
In vitro cellular assays for SKA-121 use cell lines expressing KCa3.1, such as endothelial cells, immune 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 a KCa3.1 activator.
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| Animal Protocol |
In vivo animal studies for SKA-121 would typically involve mouse models of hypertension, asthma, or inflammatory diseases. 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. Airway hyperresponsiveness is assessed in asthma models. Inflammatory markers are measured in serum and tissues. The compound's effects on vascular tone and immune cell function are evaluated. However, detailed published in vivo data are limited.
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| ADME/Pharmacokinetics |
SKA-121 is a small molecule with good cell permeability. It has a molecular weight of approximately 212.21 and a molecular formula of C12H10N2O. 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.
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| References | |
| Additional Infomation |
SKA-121 is a KCa3.1 activator with the CAS number 1820708-73-3. It exhibits EC50 values of 109 nM for KCa3.1 and 4.4 μM for KCa2.3, displaying 41-fold selectivity. It shows 200- to 400-fold selectivity over KV, NaV, and CaV1.2 channels. The compound is a positive-gating modulator that enhances Ca²⁺ sensitivity. It is a research tool for studying KCa3.1 and is not for human therapeutic use.
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| Molecular Formula |
C12H10N2O
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| Molecular Weight |
198.22060251236
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| Exact Mass |
198.079
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| CAS # |
1820708-73-3
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| PubChem CID |
91827362
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| Appearance |
White to gray solid powder
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| LogP |
3
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
15
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| Complexity |
246
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| Defined Atom Stereocenter Count |
0
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| SMILES |
NC1=NC2=CC(C)=C3C=CC=CC3=C2O1
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| InChi Key |
JEGUERWMMMQFJV-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
5-methylbenzo[g][1,3]benzoxazol-2-amine
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| Synonyms |
SKA121; SKA 121; SKA-121
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ≥ 42.86 mg/mL (~216.22 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.0449 mL | 25.2245 mL | 50.4490 mL | |
| 5 mM | 1.0090 mL | 5.0449 mL | 10.0898 mL | |
| 10 mM | 0.5045 mL | 2.5224 mL | 5.0449 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.
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