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Medchemexpress LLC Acetamide, N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]- | 893990-34-6 | 99.7% | 342.44 | 25 MG

Supplier: Medchemexpress LLC 25MGHY16689
VU 0240551 is a potent and selective neuronal K-Cl cotransporter KCC2 inhibitor with an IC50 of 560 nM, demonstrating selectivity against NKCC1. It also inhibits hERG and L-type Ca2+ channels. VU 0240551 has been shown to attenuate GABA-induced hyperpolarization of P cells, induce a positive shift in the P cell GABA reversal potential, and enhance P cell synaptic transmission.
- In HEK293 cells, VU 0240551 showed an IC50 of 568 nM for antagonist activity at KCC2.
- It exhibited an IC50 > 50 μM for antagonist activity at NKKC1 in human HEK293 cells.
- VU 0240551 reduces the P cell response to GABA in a concentration-dependent manner.
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