893990-34-6

893990-34-6 - Names and Identifiers

Name	N-(4-Methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]-acetamide
Synonyms	VU 0240551 VU0240551-1 CID 7211972 SID 56405457 VU0240551-2-D4 N-(4-Methylthiazol-2-yl)-2-(6-phenylpyridazin-3-ylthio)acetaMide N-(4-Methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide N-(4-Methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]-acetamide N-(4-Methyl-thiazol-2-yl)-2-(6-phenyl-pyridazin-3-ylsulfanyl)-acetamide
CAS	893990-34-6

893990-34-6 - Physico-chemical Properties

Molecular Formula	C16H14N4OS2
Molar Mass	342.44
Density	1.39±0.1 g/cm3(Predicted)
Melting Point	127 - 132°C
Solubility	Soluble in DMSO
Appearance	powder
Color	Pale Beige to Beige
pKa	7.59±0.50(Predicted)
Storage Condition	2-8°C
Use	VU0240551 is an inhibitor of the neuronal K-Cl cotransporter, KCC2 (IC50 = 560 nM for K+ uptake assay in KCC2-overexpressing cells). VU0240551 exhibits selectivity over the Na-K-2Cl cotransporter, NKCCl. It also inhibits hERG and L-type Ca2+ channels.
In vitro study	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.
In vivo study	VU 0240551 (10 μM) significantly blocks the chloride influx in cells from Eu rats but did not affect cells from SL rats.

893990-34-6 - Risk and Safety

WGK Germany

893990-34-6 - Reference

Reference

1: Gu W, Zhang W, Lei Y, Cui Y, Chu S, Gu X, Ma Z. Activation of spinal alpha-7 nicotinic acetylcholine receptor shortens the duration of remifentanil-induced postoperative hyperalgesia by upregulating KCC2 in the spinal dorsal horn in rats. Mol Pain. 2017 Jan-Dec;13:1744806917704769. doi: 10.1177/1744806917704769. PubMed PMID: 28425312.
2: Silvestre de Ferron B, Vilpoux C, Kervern M, Robert A, Antol J, Naassila M, Pierrefiche O. Increase of KCC2 in hippocampal synaptic plasticity disturbances after perinatal ethanol exposure. Addict Biol. 2016 Oct 25. doi: 10.1111/adb.12465. [Epub ahead of print] PubMed PMID: 27778437.
3: Chevy Q, Heubl M, Goutierre M, Backer S, Moutkine I, Eugène E, Bloch-Gallego E, Lévi S, Poncer JC. KCC2 Gates Activity-Driven AMPA Receptor Traffic through Cofilin Phosphorylation. J Neurosci. 2015 Dec 2;35(48):15772-86. doi: 10.1523/JNEUROSCI.1735-15.2015. PubMed PMID: 26631461.
4: Uwera J, Nedergaard S, Andreasen M. A novel mechanism for the anticonvulsant effect of furosemide in rat hippocampus in vitro. Brain Res. 2015 Nov 2;1625:1-8. doi: 10.1016/j.brainres.2015.08.014. Epub 2015 Aug 21. PubMed PMID: 26301821.

893990-34-6 - Preparation solution concentration reference

	1mg	5mg	10mg
1 mM	2.92 ml	14.601 ml	29.202 ml
5 mM	0.584 ml	2.92 ml	5.84 ml
10 mM	0.292 ml	1.46 ml	2.92 ml
5 mM	0.058 ml	0.292 ml	0.584 ml

Last Update：2024-01-02 23:10:35

893990-34-6 - Reference Information

biological activity

VU 0240551 is a potent inhibitor of the neuronal K-Cl cotransporter KCC2 (IC50=560 nM), selectivity compared to nkcc1. VU 0240551 also inhibits hERG and L-type Ca2 channels. VU 0240551 attenuated the GABA-induced hyperpolarization of P cells, caused a positive shift in the GABA reversal potential of P cells, and enhanced the synaptic transmission of P cells.

Last Update：2024-04-10 22:30:50