VU 0240551_product_DataBase

Bioactivity

VU 0240551 is a potent neuronal K-Cl cotransporter KCC2 inhibitor (IC50=560 nM) and is selective versus NKCC1. VU 0240551 also inhibits hERG and L-type Ca2+ channels. VU 0240551 attenuates GABA-induced hyperpolarization of P cells, produces a positive shift in the P cell GABA reversal potential and enhances P cell synaptic transmission[1][2].

Invitro

VU 0240551 reduces the P cell response to GABA in a concentration-dependent manner with 75 and 100 μM treatments causing a significant reduction in GABA-elicited hyperpolarization while 25 μM had no significant effect[2].

In Vivo

VU 0240551 (10 μM) significantly blocks the chloride influx in cells from Eu rats but did not affect cells from SL rats[3].

Name

VU 0240551

CAS

893990-34-6

Formula

C16H14N4OS2

Molar Mass

342.44

Appearance

Solid

Transport

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

Reference

[1]. Delpire E, et al. Small-molecule screen identifies inhibitors of the neuronal K-Cl cotransporter KCC2. Proc Natl Acad Sci U S A. 2009 Mar 31;106(13):5383-8. [2]. Wang Y, et al. Differential effects of GABA in modulating nociceptive vs. non-nociceptive synapses. Neuroscience. 2015;298:397-409. [3]. Balapattabi K, et al. Effects of salt-loading on supraoptic vasopressin neurones assessed by ClopHensorN chloride imaging. J Neuroendocrinol. 2019;31(8):e12752.

PeptideDB

VU 0240551

CAS: 893990-34-6 F: C16H14N4OS2 W: 342.44