| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
| ln Vitro |
The inhibitory impact of NS8593 (Compound 14) in excised patches was observed to decrease with an increase in intracellular [Ca2+] and to be equal whether the compound was supplied extracellularly or intracellularly from the cell membrane. After 100 nM apamin was applied, HEK293 cells transfected with hSK3 channels were inhibited by 80%, and by 300 nM NS8593, by 75%. By contrast, at 300 nM, NS8593 reduced the activity of mutant channels by 45%. Consequently, even with a Kd value of 0.43 µM, which is 4-fold greater than that of the wild-type hSK3 channel (Kd of 0.10 µM), NS8593 is still active on the apamin-insensitive SK3 channel. Given that the level of SK3 channel activation determines NS8593's potency, the decreased potency could be the result of the mutant channel's increased apparent Ca2+ sensitivity. At a 500 nM Ca2+ concentration, the efficacy of NS8593 dropped three times, from 0.67 µM to 2.2 µM, in line with whole-cell investigations [1].
|
|---|---|
| ln Vivo |
In C57Bl/6 mice, NS8593 (compound 14) administered intravenously at doses of 3 and 10 mg/kg has the ability to modify the rate and pattern of dopaminergic neuron firing [1].
|
| References |
|
| Molecular Formula |
C17H18CLN3
|
|---|---|
| Molecular Weight |
299.7979
|
| Exact Mass |
299.119
|
| CAS # |
875755-24-1
|
| Related CAS # |
875755-39-8;875755-24-1 (HCl);
|
| PubChem CID |
71311765
|
| Appearance |
White to off-white solid powder
|
| LogP |
4.276
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
21
|
| Complexity |
332
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
C1C[C@H](C2=CC=CC=C2C1)NC3=NC4=CC=CC=C4N3.Cl
|
| InChi Key |
VWEKCDTXUUPBNA-PFEQFJNWSA-N
|
| InChi Code |
InChI=1S/C17H17N3.ClH/c1-2-8-13-12(6-1)7-5-11-14(13)18-17-19-15-9-3-4-10-16(15)20-17;/h1-4,6,8-10,14H,5,7,11H2,(H2,18,19,20);1H/t14-;/m1./s1
|
| Chemical Name |
N-[(1R)-1,2,3,4-tetrahydronaphthalen-1-yl]-1H-benzimidazol-2-amine;hydrochloride
|
| 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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~83.33 mg/mL (~277.95 mM)
H2O : ~1 mg/mL (~3.34 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.94 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 (6.94 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.94 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3356 mL | 16.6778 mL | 33.3556 mL | |
| 5 mM | 0.6671 mL | 3.3356 mL | 6.6711 mL | |
| 10 mM | 0.3336 mL | 1.6678 mL | 3.3356 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
