Certificate of Analysis

KC 12291 hydrochloride

Name: KC 12291 hydrochloride
Brand: Alomone Labs
SKU: K-105

An Orally Effective Cardioprotective Na_V Channel Blocker

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Overview

Cat #: K-105

Lyophilized Powder yes

Source Synthetic

MW: 449.99

Purity: >97%

Effective concentration 0.5 - 100 μM.

Structure

Chemical name 3,4-Dimethoxy-N-methyl-N-[3-[(5-phenyl-1,2,4-thiadiazol-3-yl)oxy]propyl]benzeneethanamine hydrochloride.

Molecular formula C₂₂H₂₇N₃O₃S•HCl.

CAS No.: 181936-98-1

Activity Orally active voltage-gated Na⁺ (Na_V) channel blocker^1-2 with cardioprotective properties^2-4. Inhibits sustained Na⁺ currents (I_NaL) with IC₅₀ of 9.6 μM and prevents diastolic contracture in isolated atrial myocytes (IC₅₀ of about 0.7 μM)⁵.

References-Activity

Decking, U. K. et al. (1998) Naunyn. Schmiedebergs. Arch. Pharmacol. 358, 547.
Hartmann, M. et al. (1998) Naunyn. Schmiedebergs. Arch. Pharmacol. 358, 554.
Ver Donck, L. et al. (1993) Cardiovasc. Res. 27, 349.
John, G.W. et al. (2004) Cardiovasc. Drug Rev. 22, 17.
Tamareille, S. et al. (2002) J. Cardiovasc. Pharmacol. 40, 346.

Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.

Solubility DMSO. Centrifuge all product preparations before use (10000 x g 5 min).

Storage of solutions Up to four weeks at 4°C or three months at -20°C.

Our bioassay

Alomone Labs KC 12291 hydrochloride inhibits Na_V1.7 channels expressed in HEK293 cells.
A. Time course of current reversible inhibition by 50 μM KC 12291 hydrochloride (#K-105). Currents were elicited by a voltage ramp from a holding potential of -100 mV to 60 mV (30 ms) delivered every 10 seconds. B. Example traces of current response to voltage ramp stimulation before and during 50 μM KC 12291 hydrochloride application.

Scientific background

The pathophysiological importance of Na⁺ overload is highlighted by the fact that a variety of drugs reducing Na⁺ influx proved to be cardioprotective, both at the intact organ and cellular level. In addition, a correlation between the degree of Na⁺ channel blockade and functional recovery from myocardial infarction is established¹.

KC 12291 is an orally active atypical voltage-gated sodium channel blocker with cardioprotective properties^2-4. It effectively blocks cardiac voltage-gated sodium channels, involving inhibition of the peak Na⁺ current and thus delays Na⁺ overload during ischemia by enhancing the inexcitability of the heart^4-5.

KC 12291 abolishes diastolic contracture in isolated myocytes obtained from guinea-pig atria, with IC₅₀ values of 0.55 and 0.79 μM respectively, and the IC₅₀ for KC 12291 inhibition of the sustained component of Na⁺ current, I_NaL, is 9.6 μM⁶.

KC 12291 exerts a potent bradycardic effect in the rat⁷.

Target Na_V channels

Lyophilized Powder

For research purposes only, not for human use

Last Update: 07/05/2024

Specifications

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Scientific Background

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