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Cat. No. M20808
ML277 Structure


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Biological Activity

ML277 (CID-53347902) is a potent activator of KCNQ1 channels with an EC50 of 260 nM and shows >100-fold selectivity over KCNQ2 and KCNQ4.

Chemical Information
Molecular Weight 471.59
Formula C23H25N3O4S2
CAS Number 1401242-74-7
Solubility (25°C) DMSO 94 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.


[1] Demin Ma, et al. Proc Natl Acad Sci U S A. Structural mechanisms for the activation of human cardiac KCNQ1 channel by electro-mechanical coupling enhancers

[2] Xinle Zou, et al. Front Physiol. Pharmacological rescue of specific long QT variants of KCNQ1/KCNE1 channels

[3] Katrien Willegems, et al. Nat Commun. Structural and electrophysiological basis for the modulation of KCNQ1 channel currents by ML277

[4] Jodene Eldstrom, et al. J Gen Physiol. ML277 regulates KCNQ1 single-channel amplitudes and kinetics, modified by voltage sensor state

[5] Panpan Hou, et al. Elife. ML277 specifically enhances the fully activated open state of KCNQ1 by modulating VSD-pore coupling

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Keywords: ML277, CID-53347902 supplier, Potassium Channel, inhibitors, activators

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