An activator of KCNQ1
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ML-277

Item No. 15193

Technical Information
Formal Name
(2R)-N-[4-(4-methoxyphenyl)-2-thiazolyl]-1-[(4-methylphenyl)sulfonyl]-2-piperidinecarboxamide
CAS Number
1401242-74-7
Synonyms
  • CID-53347902
Molecular Formula
C23H25N3O4S2
Formula Weight
Purity
≥95%
Formulation
A crystalline solid
λmax
242, 270 nm
SMILES
COC1=CC=C(C2=CSC(NC([C@H]3CCCCN3S(C4=CC=C(C)C=C4)(=O)=O)=O)=N2)C=C1
InChi Code
InChI=1S/C23H25N3O4S2/c1-16-6-12-19(13-7-16)32(28,29)26-14-4-3-5-21(26)22(27)25-23-24-20(15-31-23)17-8-10-18(30-2)11-9-17/h6-13,15,21H,3-5,14H2,1-2H3,(H,24,25,27)/t21-/m1/s1
InChi Key
OXQNLLVUVDAEHC-OAQYLSRUSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    ML-277 is a potent activator of KCNQ1 channels (EC50 = 260 nM).1 The EC50 value of this compound at the related channels KCNQ2, KCNQ4, and hERG exceeds 30 µM.1 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.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Mattmann, M.E., Yu, H., Lin, Z., et alIdentification of (R)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-1-tosylpiperidine-2-carboxamide, ML277, as a novel, potent and selective Kv7.1 (KCNQ1) potassium channel activator. Bioorg. Med. Chem. Lett. 22(18), 5936-5941 (2012).

    2. Yu, H., Lin, Z., Mattmann, M.E., et alDynamic subunit stoichiometry confers a progressive continuum of pharmacological sensitivity by KCNQ potassium channels. Proc. Natl. Acad. Sci. USA 110(21), 8732-8737 (2013).