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Merck

SML0524

Sigma-Aldrich

ML277

≥98% (HPLC)

Sinónimos:

(2R)-N-[4-(4-Methoxyphenyl)-1,3-thiazol-2-yl]-1-(4-methylphenyl)sulfonylpiperidine-2-carboxamide, (R)-N-(4-(4-Methoxyphenyl)thiazol-2-yl)-1-tosylpiperidine-2-carboxamide, CID-53347902, VU0458298-2, VU0458298-3

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About This Item

Fórmula empírica (notación de Hill):
C23H25N3O4S2
Número de CAS:
Peso molecular:
471.59
Número MDL:
Código UNSPSC:
12352200
ID de la sustancia en PubChem:
NACRES:
NA.77

Nivel de calidad

Ensayo

≥98% (HPLC)

Formulario

powder

color

white to beige

solubilidad

DMSO: 5 mg/mL, clear

temp. de almacenamiento

2-8°C

cadena SMILES

COc1ccc(cc1)-c2cnc(NC(=O)[C@H]3CCCCN3S(=O)(=O)c4ccc(C)cc4)s2

InChI

1S/C23H25N3O4S2/c1-16-6-12-19(13-7-16)32(28,29)26-14-4-3-5-20(26)22(27)25-23-24-15-21(31-23)17-8-10-18(30-2)11-9-17/h6-13,15,20H,3-5,14H2,1-2H3,(H,24,25,27)/t20-/m1/s1

Clave InChI

UKSXJENCMIVQMU-HXUWFJFHSA-N

Aplicación

ML277 has been used as the KCNQ1 activator to treat cells in lung metastasis assay.

Acciones bioquímicas o fisiológicas

ML277 is a potent activator of KCNQ1 (Kv7.1) channels with >100-fold selectivity versus KCNQ2 and KCNQ4 and no activity against the hERG potassium channel up to 30 μM. KCNQ1 is a voltage-gated potassium channel required for repolarization phase of the cardiac action potential. Mutations in the KCNQ1 gene are associated with long QT syndrome (LQTS), a disorder in which the heart muscles take longer than normal to recover after each heart beat and can lead to dangerous arrhythmias such as atrial fibrillation. Activators of KCNQ1 channels could have potential use in treatments of LQTS. ML277 is the first selective and potent activator found, with an EC50 of 260 nM.
ML277 is a potent activator of KCNQ1 (Kv7.1) channels with >100-fold selectivity versus KCNQ2 and KCNQ4.

Características y beneficios

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.

Pictogramas

Exclamation mark

Palabra de señalización

Warning

Frases de peligro

Clasificaciones de peligro

Acute Tox. 4 Oral - Eye Irrit. 2

Código de clase de almacenamiento

11 - Combustible Solids

Clase de riesgo para el agua (WGK)

WGK 3

Punto de inflamabilidad (°F)

Not applicable

Punto de inflamabilidad (°C)

Not applicable


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Gaelle Lentini et al.
PloS one, 12(12), e0189556-e0189556 (2017-12-16)
During the infection process, Apicomplexa discharge their secretory organelles called micronemes, rhoptries and dense granules to sustain host cell invasion, intracellular replication and to modulate host cell pathways and immune responses. Herein, we describe the Toxoplasma gondii Deg-like serine protein
Hypermethylated KCNQ1 acts as a tumor suppressor in hepatocellular carcinoma
Fan H, et al.
Biochemical and Biophysical Research Communications, 503(4), 3100-3107 (2018)
Jun Ho Lee et al.
Pflugers Archiv : European journal of physiology, 472(1), 89-102 (2020-01-11)
The group of KCNQ-encoded voltage-gated potassium (Kv7) channels includes five family members (Kv7.1-7.5). We examined the molecular expression and functional roles of Kv7 channels in corporal smooth muscle (CSM). Isolated rabbit CSM strips were mounted in an organ bath system
Dmitry Tsvetkov et al.
British journal of pharmacology, 174(2), 150-162 (2016-12-22)
K We used Kcnq1 R-L3 produced similar concentration-dependent relaxations (EC We conclude that K
Xiaohong Wei et al.
PloS one, 13(3), e0192122-e0192122 (2018-03-27)
Pre-eclampsia is associated with altered maternal and placental vascular reactivity. Kv7 channels (encoded by KCNQ 1-5 genes) are a potential contributor to the regulation of vascular tone in CPAs (chorionic plate arteries) during normal pregnancy. The aim of this study

Artículos

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We offer many products related to potassium channels for your research needs.

We offer many products related to potassium channels for your research needs.

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