893990-34-6
Chemical Structure
VU 0240551
- CAS No.: 893990-34-6
- Formula:C16H14N4OS2
- Molecular Weight:342.44
IUPAC Name: N-(4-methylthiazol-2-yl)-2-((6-phenylpyridazin-3-yl)thio)acetamide
InChIKey: WJRWSLORVIHRNX-UHFFFAOYSA-N
SMILES: O=C(CSC1=NN=C(C2=CC=CC=C2)C=C1)NC3=NC(C)=CS3
Biological Activity: 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].
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VU 0240551 | 99.70% | 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. | ||||||||||||||||||||
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- [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. [Content Brief]
- [2]. Wang Y, et al. Differential effects of GABA in modulating nociceptive vs. non-nociceptive synapses. Neuroscience. 2015;298:397-409. [Content Brief]
Keywords
