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Purity: ≥98%
NS-11021 is a novel, potent and selective activator of large-conductance Ca2+-activated potassium channels (BKCa, KCa1.1). BK channel activation by NS11021 decreases excitability and contractility of urinary bladder smooth muscle. NS11021 enhances erectile responses in rats.
| ln Vitro |
At a concentration of 3 μM, NS 11021 (1-30 μM) increases hKCa1.1 current from 2 μA to 4 μA and can dose-dependently activate hKCa1.1 channels in X. laevis eggs. The channel's hKCa1.1 current is increased by 171% by NS 11021 (3 μM), causing it to alternate between open and closed structures on a regular basis. NS 11021 (0-10 μM), a channel in X that keeps its structure closed. monoclonal HEK293 cells that consistently express hKCa1.1 can have their hKCa1.1 currents enhanced by laevis oocytes in a concentration-dependent way [1]. The frog gastrocnemius muscle's resting membrane potential (RMP) was unaffected by NS 11021 (5 or 50 μM, which increased current by 187%[1] M), but the action potential (AP) rise time was markedly and dose-dependently increased. Completely reversing the death of the upper stage of the AP complex caused by hydrogen peroxide in dividing myofibers, NS 11021 (1 μM) Attenuates the effects of CS+RW in Proximal Renal Renal Kubular Epithelial (NRK) cells (Cold for 18 hours and Rewarmed for 2 hours) on conductive mitoBK channels. cell death, depolarization, generation of superoxide, and respiratory failure [3].
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| References |
[1]. Bo Hjorth Bentzen, et al. The small molecule NS11021 is a potent and specific activator of Ca2+-activated big-conductance K+ channels. Mol Pharmacol. 2007 Oct;72(4):1033-44
[2]. Cagil Coskun, et al. BK channel openers NS1619 and NS11021 reverse hydrogen peroxide-induced membrane potential changes in skeletal muscle. J Recept Signal Transduct Res. 2020 Oct;40(5):449-455. [3]. Stephen Shrum, et al. Specific BK Channel Activator NS11021 Protects Rat Renal Proximal Tubular Cells from Cold Storage-Induced Mitochondrial Injury In Vitro. Biomolecules. 2019 Dec 4;9(12):825. |
| Molecular Formula |
C16H9BRF6N6S
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|---|---|
| Molecular Weight |
511.2444
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| Exact Mass |
509.9697
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| Elemental Analysis |
C, 37.59; H, 1.77; Br, 15.63; F, 22.30; N, 16.44; S, 6.27
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| CAS # |
956014-19-0
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| Related CAS # |
956014-19-0;
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| Appearance |
Solid powder
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| SMILES |
S=C(NC1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1)NC2=CC=C(Br)C=C2C3=NNN=N3
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| InChi Key |
INVIVOAFDIKYQMOMF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H9BrF6N6S/c17-9-1-2-12(11(6-9)13-26-28-29-27-13)25-14(30)24-10-4-7(15(18,19)20)3-8(5-10)16(21,22)23/h1-6H,(H2,24,25,30)(H,26,27,28,29)
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| Chemical Name |
N'-[3,5-bis(trifluoromethyl)phenyl]-N-[4-bromo-2-(2H-tetrazol-5-yl)phenyl]-thiourea
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| Synonyms |
NS-11021 NS 11021 NS11021.
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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 (~195.60 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.07 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 20.8 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: ≥ 2.08 mg/mL (4.07 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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9560 mL | 9.7801 mL | 19.5603 mL | |
| 5 mM | 0.3912 mL | 1.9560 mL | 3.9121 mL | |
| 10 mM | 0.1956 mL | 0.9780 mL | 1.9560 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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