| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
In pig endothelial cells, SKA-111 (1 μM, 5 min) causes KCa3.1 membrane hyperischemia [1]. In porcine major coronary arteries (PCA), SKA-111 (1 μM, 5 min) greatly enhances the Bradykinin-induced endothelium-derived minimum (EDH)-type relaxation [1].
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|---|---|
| ln Vivo |
In isolated stent hearts, Bradykinin-induced coronary arterial dilatation is improved by SKA-111 (1 μM for cardiac perfusion) [1].
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| Animal Protocol |
Animal/Disease Models: Langendorff[1] in rat heart
Doses: 1 μM Route of Administration: Cardiac perfusion Experimental Results: Significant enhancement of 1 nM BK-induced coronary perfusion pressure in the presence of vasoconstrictors in isolated rat hearts (CPP) decline. |
| References |
[1]. Oliván-Viguera A, et.al. Vascular Reactivity Profile of Novel KCa 3.1-Selective Positive-Gating Modulators in the Coronary Vascular Bed. Basic Clin Pharmacol Toxicol. 2016 Aug;119(2):184-92.
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| Molecular Formula |
C12H10N2S
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|---|---|
| Molecular Weight |
214.286201000214
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| Exact Mass |
214.05
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| Elemental Analysis |
C, 67.26; H, 4.70; N, 13.07; S, 14.96
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| CAS # |
1369170-24-0
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| Related CAS # |
1369170-24-0;
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| PubChem CID |
82549899
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| Appearance |
Solid powder
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| LogP |
3.6
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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 |
S1C(N)=NC2=C1C=C(C)C1C=CC=CC=12
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| InChi Key |
JQZQMZXXJFFVFE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H10N2S/c1-7-6-10-11(14-12(13)15-10)9-5-3-2-4-8(7)9/h2-6H,1H3,(H2,13,14)
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| Chemical Name |
5-methylbenzo[e][1,3]benzothiazol-2-amine
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| Synonyms |
SKA-111 SKA111 SKA 111
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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 : ~100 mg/mL (~466.66 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.67 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.6666 mL | 23.3329 mL | 46.6657 mL | |
| 5 mM | 0.9333 mL | 4.6666 mL | 9.3331 mL | |
| 10 mM | 0.4667 mL | 2.3333 mL | 4.6666 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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