A potent activator of KCNQ1 (Kv7.1) channels (EC50 = 260 nM); EC50 > 30 µM for KCNQ2

ML-277 – 10 mg

Brand:
Cayman
CAS:
1401242-74-7
Storage:
-20
UN-No:
Non-Hazardous - /

Potassium (K+) channels are categorized by their mode of activation and the number of transmembrane segments.{24547} The voltage-gated six-transmembrane K+ channels include KCNQ1, first recognized for its role in cardiac function and subsequently in hearing, gastrointestinal chloride secretion, and other processes.{24547,24548} ML-277 is a potent activator of KCNQ1 channels (EC50 = 260 nM).{24545} The EC50 value of this compound at the related channels KCNQ2, KCNQ4, and hERG exceeds 30 µM.{24545} ML-277 potentiates both homomultimeric KCNQ1 channels and unsaturated heteromultimeric (KCNQ1/KCNE1) channels in model cardiomyocytes and augments delayed rectifier K+ current in cultured human cardiomyocytes.{24546}  

 

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Description

A potent activator of KCNQ1 (Kv7.1) channels (EC50 = 260 nM); EC50 > 30 µM for KCNQ2, KCNQ4, and hERG; potentiates both homomultimeric KCNQ1 channels and unsaturated heteromultimeric (KCNQ1/KCNE1) channels in model cardiomyocytes and augments IKs current in cultured human cardiomyocytes

Formal name: (2R)-N-[4-(4-methoxyphenyl)-2-thiazolyl]-1-[(4-methylphenyl)sulfonyl]-2-piperidinecarboxamide

Synonyms:  CID-53347902

Molecular weight: 471.6

CAS: 1401242-74-7

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Activators||Research Area|Cardiovascular System|Heart

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