ML277 Property

Density 

1.341±0.06 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

DMSO: 5 mg/ml

form 

powder

pka

8.37±0.70(Predicted)

color 

white to beige

Safety

Hazard Codes 

Xn

Risk Statements 

22-36

Safety Statements 

26

WGK Germany 

3

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P337+P313IF eye irritation persists: Get medical advice/attention.

ML277 Chemical Properties,Usage,Production

Description

Potassium (K⁺) channels are categorized by their mode of activation and the number of transmembrane segments. 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. ML-277 is a potent activator of KCNQ1 channels (EC₅₀ = 260 nM). The EC₅₀ value of this compound at the related channels KCNQ2, KCNQ4, and hERG exceeds 30 μM. 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.

Uses

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

Biochem/physiol Actions

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.

storage

Store at -20°C