A2764 2HCl

A2764 dihydrochloride is a selective inhibitor of TRESK (KCNK18) with an IC50 value of 11.8 μM. A2764 can inhibit TRESK in native cells, leading to cell depolarization and increased excitability.

Product information

CAS Number: 861038-72-4

Molecular Weight: 351.70

Formula: C15H21Cl3N2O

Chemical Name: {2-[(5-chloroquinolin-8-yl)oxy]ethyl}diethylamine dihydrochloride

Smiles: Cl.Cl.CCN(CCOC1=CC=C(Cl)C2=CC=CN=C12)CC

InChiKey: ZVRDPULCSHGKBD-UHFFFAOYSA-N

InChi: InChI=1S/C15H19ClN2O.2ClH/c1-3-18(4-2)10-11-19-14-8-7-13(16)12-6-5-9-17-15(12)14;;/h5-9H,3-4,10-11H2,1-2H3;2*1H

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 41.67 mg/mL (118.48 mM; Need ultrasonic)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

A2764 (100 µM) inhibits the background K+ current by 42.8±11.5% when it applies to the oocytes expressing mTRESK. A2764 (100 µM) shows an improved inhibitory potency for activated channel with an IC50 of activated channel in ionomycin-activated mTRESK current.The subsequent application of A2764 strongly inhibits the current (77.8±3.5%). A2764 (100 µM) inhibits the current of TRESK under resting conditions and in the activated state by 42.8±11.5% and 77.8±3.5%, respectively.

References:

1. Lengyel M, et al. Chemically Modified Derivatives of the Activator Compound Cloxyquin Exert Inhibitory Effect on TRESK (K2P18.1) Background Potassium Channel.Mol Pharmacol. 2019 Jun;95(6):652-660.

Products are for research use only. Not for human use.