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Merck

X2254

XE-991

≥98% (HPLC), powder, KCNQ channel blocker

Sinónimos:

10,10-bis(4-pyridinylmethyl)-9(10H)-anthracenone

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Acerca de este artículo

Fórmula empírica (notación de Hill):
C26H20N2O
Número CAS:
Peso molecular:
376.45
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
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Nombre del producto

XE-991, ≥98% (HPLC)

SMILES string

O=C1c2ccccc2C(Cc3ccncc3)(Cc4ccncc4)c5ccccc15

InChI key

KHJFBUUFMUBONL-UHFFFAOYSA-N

InChI

1S/C26H20N2O/c29-25-21-5-1-3-7-23(21)26(17-19-9-13-27-14-10-19,18-20-11-15-28-16-12-20)24-8-4-2-6-22(24)25/h1-16H,17-18H2

assay

≥98% (HPLC)

color

white to beige

solubility

DMSO: >20 mg/mL

originator

Merck & Co., Inc., Kenilworth, NJ, U.S.

storage temp.

2-8°C

Quality Level

Application

XE-991 has been used as a KCNQ (Kv7.2/7.3) inhibitor to examine whether M-current inhibition affects oxytocin receptor (TGOT) mediated depolarization. It has also been used as an KCNQ inhibitor to study the ionic mechanism responsible for the overshoot/undershoot in membrane potential in mouse cholinergic interneurons (ChIs) in the presence of tetrodotoxin (TTX).

Biochem/physiol Actions

XE-991 is a KCNQ channel blocker.
XE-991 is a KCNQ channel blocker; which is more potent than linopiridine (Cat. No. L-134).

Features and Benefits

This compound is featured on the Potassium Channels page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound was developed by Merck & Co., Inc., Kenilworth, NJ, U.S.. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

pictograms

Exclamation mark

signalword

Warning

Hazard Classifications

Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

target_organs

Respiratory system

Clase de almacenamiento

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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Oxytocin transforms firing mode of CA2 hippocampal neurons
Tirko N, et al.
Neuron, 100(3), 593-608 (2018)
David Bartolomé-Martín et al.
Neuropharmacology, 161, 107568-107568 (2019-03-20)
Dopamine and glutamate transporters (DAT and GLT-1, respectively) share some biophysical characteristics, as both are secondary active carriers coupled to electrochemical ion gradients. In order to identify common or specific components of their respective proteomes, we performed a proximity labelling
Pauses in cholinergic interneuron activity are driven by excitatory input and delayed rectification, with dopamine modulation
Zhang Y, et al.
Neuron, 98(5), 918-925 (2018)
Lena Rubi et al.
Neuromolecular medicine, 15(3), 476-492 (2013-05-23)
Neuronal L-type voltage-gated calcium channels (LTCCs) are involved in several physiological functions, but increased activity of LTCCs has been linked to pathology. Due to the coupling of LTCC-mediated Ca(2+) influx to Ca(2+)-dependent conductances, such as KCa or non-specific cation channels
Yusuf Olgar et al.
Journal of cellular physiology, 237(2), 1353-1371 (2021-10-12)
Insufficient-heart function is associated with myocardial insulin resistance in the elderly, particularly associated with long-QT, in a dependency on dysfunctional KCNQ1/KCNE1-channels. So, we aimed to examine the contribution of alterations in KCNQ1/KCNE1-current (IKs ) to the aging-related remodeling of the heart

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