A KCC2 inhibitor (IC50 = 568 nM); selectively inhibits KCC2 over NKCC1 (IC50 = >50 µM) but does inhibit the activity of adenosine A1 and A3 receptors

VU0240551 – 25 mg

Brand:
Cayman
CAS:
893990-34-6
Storage:
-20
UN-No:
Non-Hazardous - /

VU0240551 is a K+/Cl- cotransporter 2 (KCC2) inhibitor (IC50 = 568 nM).{46717} It selectively inhibits KCC2 over Na+/K+/Cl- cotransporter 1 (NKCC1; IC50 = >50 µM) but does inhibit the activity of adenosine A1 and A3 receptors, as well as inhibits activity of L-type calcium channels at the benzothiazepine site and human ether-a-go-go-related gene (hERG) potassium channels by greater than 50% in a panel of 68 receptors, ion channels, and transporters at 10 µM. VU0240551 decreases potassium ion uptake by 70% in HEK293 cells expressing KCC2 when used at a concentration of 1 µM.  

 

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SKU: 29790 - 25 mg Category:

Description

A KCC2 inhibitor (IC50 = 568 nM); selectively inhibits KCC2 over NKCC1 (IC50 = >50 µM) but does inhibit the activity of adenosine A1 and A3 receptors, as well as inhibits activity of L-type calcium channels at the benzothiazepine site and hERG potassium channels by >50% in a panel at 10 µM; decreases potassium ion uptake by 70% in HEK293 cells expressing KCC2 at 1 µM

Formal name: N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]-acetamide

Synonyms: 

Molecular weight: 342.4

CAS: 893990-34-6

Purity: ≥98%

Formulation: A crystalline solid

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