NS8593 hydrochloride

Name: NS8593 hydrochloride
Brand: MedChemExpress
SKU: HY-110105
Rating: 4.5 (1 reviews)

Cat. No.: HY-110105 Purity: 99.81%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

NS8593 hydrochloride is a potent and selective small conductance Ca²⁺-activated K⁺ channels (SK channels) inhibitor. NS8593 hydrochloride reversibly inhibits SK3-mediated currents with a K_d value of 77 nM. NS8593 hydrochloride inhibits all the SK1-3 subtypes Ca²⁺-dependently (K_ds of 0.42, 0.60, and 0.73 μM, respectively, at 0.5 μM Ca²⁺), and does not affect the Ca²⁺-activated K⁺ channels of intermediate and large conductance (hIK and hBK channels, respectively).

For research use only. We do not sell to patients.

NS8593 hydrochloride Chemical Structure

CAS No. : 875755-24-1

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 121	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 121	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 110	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 215	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 495	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

Kd: 0.42 μM (SK1), 0.60 μM (SK2) , and 0.73 μM (SK3)^[2]

In Vitro

When tested in excised patches, it is found that the inhibition by NS8593 (compound 14) decreased as the intracellular [Ca²⁺] is increased and that NS8593 is equipotent when applied from either the intracellular or the extracellular side of the cell membrane. A HEK293 cell transiently transfected with hSK3 channels is inhibited by 80% upon application of 100 nM apamin and by 75% after application of 300 nM NS8593. In contrast, NS8593 inhibits the mutated channel by 45% at 300 nM. NS8593 thus remains active on the apamin-insensitive SK3 channel, although the K_d value of 0.43 μM is 4-fold higher than found for a wild-type hSK3 channel (K_d of 0.10 μM). As the potency of NS8593 is dependent on the degree of SK3 channel activation, the decreased potency could thus reflect an increased apparent Ca²⁺-sensitivity of the mutated channels. Similar to the whole-cell experiments, the potency of NS8593 is reduced 3-fold from 0.67 μM to 2.2 μM when tested at a Ca²⁺ concentration of 500 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

NS8593 (compound 14) (3 and 10 mg/kg intravenously) is able to affect firing rate and firing pattern of dopaminergic neurons in vivo in C57Bl/6 mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

299.80

Formula

C₁₇H₁₈ClN₃

CAS No.

875755-24-1

Appearance

Solid

Color

White to off-white

SMILES

[H]Cl.C1(N[C@@H]2CCCC3=C2C=CC=C3)=NC4=CC=CC=C4N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 83.33 mg/mL (277.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 1 mg/mL (3.34 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (6.94 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.94 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (6.94 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.81%

Select Batch:

Data Sheet (279 KB) SDS (252 KB)

COA (254 KB) LCMS (269 KB)

Handling Instructions (2659 KB)

References

[1]. Sørensen US, et al. Synthesis and structure-activity relationship studies of 2-(N-substituted)-aminobenzimidazoles as potent negative gating modulators ofsmall conductance Ca2+-activated K+ channels. J Med Chem. 2008 Dec 11;51(23):7625-34. [Content Brief]

[2]. Strøbaek D, et al. Inhibitory gating modulation of small conductance Ca2+-activated K+ channels by the synthetic compound (R)-N-(benzimidazol-2-yl)-1,2,3,4-tetrahydro-1-naphtylamine (NS8593) reduces afterhyperpolarizing current in hippocampal CA1 neurons. Mol Pharmacol. 2006 Nov;70(5):1771-82. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	3.3356 mL	16.6778 mL	33.3556 mL	83.3889 mL
DMSO	5 mM	0.6671 mL	3.3356 mL	6.6711 mL	16.6778 mL
	10 mM	0.3336 mL	1.6678 mL	3.3356 mL	8.3389 mL
	15 mM	0.2224 mL	1.1119 mL	2.2237 mL	5.5593 mL
	20 mM	0.1668 mL	0.8339 mL	1.6678 mL	4.1694 mL
	25 mM	0.1334 mL	0.6671 mL	1.3342 mL	3.3356 mL
	30 mM	0.1112 mL	0.5559 mL	1.1119 mL	2.7796 mL
	40 mM	0.0834 mL	0.4169 mL	0.8339 mL	2.0847 mL
	50 mM	0.0667 mL	0.3336 mL	0.6671 mL	1.6678 mL
	60 mM	0.0556 mL	0.2780 mL	0.5559 mL	1.3898 mL
	80 mM	0.0417 mL	0.2085 mL	0.4169 mL	1.0424 mL
	100 mM	0.0334 mL	0.1668 mL	0.3336 mL	0.8339 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.