| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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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].
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| 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].
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| References |
| 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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