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SML1368

Sigma-Aldrich

CLP257

≥98% (HPLC)

Sinónimos:

(5Z)-5-[(4-Fluoro-2-hydroxyphenyl)methylene]-2-(tetrahydro-1-(2H)-pyridazinyl)-4(5H)-thiazolone

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About This Item

Fórmula empírica (notación de Hill):
C14H14FN3O2S
Número de CAS:
1181081-71-9
Peso molecular:
307.34
MDL number:
MFCD28166488
UNSPSC Code:
12352200
PubChem Substance ID:
329825822
NACRES:
NA.77

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

, white to yellow to light brown

solubility

DMSO: 20 mg/mL, clear

storage temp.

2-8°C

SMILES string

O=C1/C(SC(N2CCCCN2)=N1)=C/C3=CC=C(F)C=C3O

InChI

1S/C14H14FN3O2S/c15-10-4-3-9(11(19)8-10)7-12-13(20)17-14(21-12)18-6-2-1-5-16-18/h3-4,7-8,16,19H,1-2,5-6H2/b12-7-

InChI key

SKCADXVKQRCWTR-GHXNOFRVSA-N

Application

CLP257 has been used as a K+- Cl- cotransporter 2 (KCC2) enhancer in human neuron culture.

Biochem/physiol Actions

CLP257 is a selective K+-Cl− cotransporter KCC2 activator that restored impaired Cl− transport in neurons with reduced KCC2 activity. Apparently, CLP257 modulates plasmalemmal KCC2 protein turnover post-translationally.
In streptozotocin treated rats, by activating a K+- Cl- cotransporter 2 (KCC2) in the arginine-vasopressin neuron, CLP257 mediates γ-aminobutyric acid (GABA)ergic excitation. It is however inactive with KCC1, KCC3 and KCC4.

pictograms

Exclamation mark
GHS07

signalword

Warning

hcodes

H302

Hazard Classifications

Acute Tox. 4 Oral

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificados de análisis (COA)

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Young-Beom Kim et al.
Diabetes, 67(3), 486-495 (2017-12-08)
Diabetes mellitus (DM) is associated with increased plasma levels of arginine-vasopressin (AVP), which may aggravate hyperglycemia and nephropathy. However, the mechanisms by which DM may cause the increased AVP levels are not known. Electrophysiological recordings in supraoptic nucleus (SON) slices
Aaron J Barbour et al.
Neurobiology of disease, 141, 104878-104878 (2020-04-29)
Approximately half of people infected with HIV (PWH) exhibit HIV-associated neuropathology (neuroHIV), even when receiving combined antiretroviral therapy. Opiate use is widespread in PWH and exacerbates neuroHIV. While neurons themselves are not infected, they incur sublethal damage and GABAergic disruption
Martin Gagnon et al.
Nature medicine, 19(11), 1524-1528 (2013-10-08)
The K(+)-Cl(-) cotransporter KCC2 is responsible for maintaining low Cl(-) concentration in neurons of the central nervous system (CNS), which is essential for postsynaptic inhibition through GABA(A) and glycine receptors. Although no CNS disorders have been associated with KCC2 mutations

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