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Merck
CN

SML1368

CLP257

≥98% (HPLC)

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):
C14H14FN3O2S
CAS Number:
1181081-71-9
Molecular Weight:
307.34
NACRES:
NA.77
PubChem Substance ID:
329825822
UNSPSC Code:
12352200
MDL number:
MFCD28166488
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
100

Key Documents

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Product Name

CLP257, ≥98% (HPLC)

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-

SMILES string

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

InChI key

SKCADXVKQRCWTR-GHXNOFRVSA-N

assay

≥98% (HPLC)

form

powder

color

, white to yellow to light brown

solubility

DMSO: 20 mg/mL, clear

storage temp.

2-8°C

Quality Level

100

Related Categories

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.
CLP257 is a selective K+-Cl− cotransporter KCC2 activator.
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

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000211075
0000211075
0000211074
0000211074
0000155047

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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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