VU 0240551
Modify Date: 2024-01-03 19:12:01
VU 0240551 structure
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Common Name | VU 0240551 | ||
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| CAS Number | 893990-34-6 | Molecular Weight | 342.43900 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C16H14N4OS2 | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | N/A | |
Use of VU 0240551VU 0240551 is a small molecule inhibitor of the neuronal K-Cl cotransporter, KCC2 (IC50 = 560 nM for K+ uptake assay in KCC2-overexpressing cells).IC50 value: 560 nM [1]Target: K-Cl cotransporter(KCC2)VU 0240551 exhibits selectivity over the Na-K-2Cl cotransporter, NKCCl. VU 0240551 also inhibits hERG and L-type Ca2+ channels [1]. Herein we report the discovery and SAR of an improved novel antagonist (VU0463271) of the neuronal-specific potassium-chloride cotransporter 2 (KCC2), with an IC(50) of 61 nM and >100-fold selectivity versus the closely related Na-K-2Cl cotransporter 1 (NKCC1) and no activity in a larger panel of GPCRs, ion channels and transporters [2]. |
| Name | N-(4-methyl-1,3-thiazol-2-yl)-2-(6-phenylpyridazin-3-yl)sulfanylacetamide |
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| Synonym | More Synonyms |
| Description | VU 0240551 is a small molecule inhibitor of the neuronal K-Cl cotransporter, KCC2 (IC50 = 560 nM for K+ uptake assay in KCC2-overexpressing cells).IC50 value: 560 nM [1]Target: K-Cl cotransporter(KCC2)VU 0240551 exhibits selectivity over the Na-K-2Cl cotransporter, NKCCl. VU 0240551 also inhibits hERG and L-type Ca2+ channels [1]. Herein we report the discovery and SAR of an improved novel antagonist (VU0463271) of the neuronal-specific potassium-chloride cotransporter 2 (KCC2), with an IC(50) of 61 nM and >100-fold selectivity versus the closely related Na-K-2Cl cotransporter 1 (NKCC1) and no activity in a larger panel of GPCRs, ion channels and transporters [2]. |
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| Related Catalog | |
| References |
| Molecular Formula | C16H14N4OS2 |
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| Molecular Weight | 342.43900 |
| Exact Mass | 342.06100 |
| PSA | 124.80000 |
| LogP | 4.28880 |
| Storage condition | 2-8℃ |
| RIDADR | NONH for all modes of transport |
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Chloride dysregulation and inhibitory receptor blockade yield equivalent disinhibition of spinal neurons yet are differentially reversed by carbonic anhydrase blockade.
Pain 156 , 2431-7, (2015) Synaptic inhibition plays a key role in processing somatosensory information. Blocking inhibition at the spinal level is sufficient to produce mechanical allodynia, and many neuropathic pain condition... |
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Efficacy of synaptic inhibition depends on multiple, dynamically interacting mechanisms implicated in chloride homeostasis.
PLoS Comput. Biol. 7 , e1002149, (2011) Chloride homeostasis is a critical determinant of the strength and robustness of inhibition mediated by GABA(A) receptors (GABA(A)Rs). The impact of changes in steady state Cl(-) gradient is relativel... |
| VU 0240551 |