1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. NS8593 hydrochloride

NS8593 hydrochloride 

Cat. No.: HY-110105 Purity: 99.88%
Handling Instructions

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 Kd value of 77 nM. NS8593 hydrochloride inhibits all the SK1-3 subtypes Ca2+-dependently (Kds 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

NS8593 hydrochloride Chemical Structure

CAS No. : 875755-24-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1  mL in DMSO USD 110 In-stock
Estimated Time of Arrival: December 31
5 mg USD 100 In-stock
Estimated Time of Arrival: December 31
10 mg USD 195 In-stock
Estimated Time of Arrival: December 31
25 mg USD 450 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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 Kd value of 77 nM. NS8593 hydrochloride inhibits all the SK1-3 subtypes Ca2+-dependently (Kds 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)[1][2].

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 Kd value of 0.43 µM is 4-fold higher than found for a wild-type hSK3 channel (Kd 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].

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].

Molecular Weight

299.80

Formula

C₁₇H₁₈ClN₃

CAS No.

875755-24-1

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 83.33 mg/mL (277.95 mM; Need ultrasonic)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (6.94 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

NS8593NS 8593NS-8593Potassium ChannelKcsASK1SK2SK3channeldopaminergicneuronsneurologicalhIKhBKCa2+Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
NS8593 hydrochloride
Cat. No.:
HY-110105
Quantity:
MCE Japan Authorized Agent: